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MX365986B - Derivativos de piperidina fusionados con espiro para usarse como inhibidores del canal de potasio medular externo renal. - Google Patents

Derivativos de piperidina fusionados con espiro para usarse como inhibidores del canal de potasio medular externo renal.

Info

Publication number
MX365986B
MX365986B MX2015001115A MX2015001115A MX365986B MX 365986 B MX365986 B MX 365986B MX 2015001115 A MX2015001115 A MX 2015001115A MX 2015001115 A MX2015001115 A MX 2015001115A MX 365986 B MX365986 B MX 365986B
Authority
MX
Mexico
Prior art keywords
inhibitors
spiro
potassium channel
piperidine derivatives
outer medullary
Prior art date
Application number
MX2015001115A
Other languages
English (en)
Other versions
MX2015001115A (es
Inventor
Yang Yu
Alexander Pasternak
Jinlong Jiang
Takao Suzuki
Haifeng Tang
Xin Gu
Zhicai Wu
Shuzhi Dong
Fa-Xiang Ding
Jessica Frie
Original Assignee
Merck Sharp & Dohme
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
Priority claimed from PCT/CN2012/079184 external-priority patent/WO2014015495A1/en
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of MX2015001115A publication Critical patent/MX2015001115A/es
Publication of MX365986B publication Critical patent/MX365986B/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4995Pyrazines or piperazines forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención proporciona compuestos de Fórmula I (ver Fórmula) y las sales farmacéuticamente aceptables del mismo, que son inhibidores del canal de ROMK (Kir1.1); los compuestos se pueden usar como agentes diuréticos y/o natriuréticos y para la terapia y la profilaxis de afecciones médicas que incluyen enfermedades cardiovasculares tales como hipertensión, insuficiencia cardíaca y afecciones asociadas con excesiva retención de sal y agua.
MX2015001115A 2012-07-26 2013-07-25 Derivativos de piperidina fusionados con espiro para usarse como inhibidores del canal de potasio medular externo renal. MX365986B (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
PCT/CN2012/079184 WO2014015495A1 (en) 2012-07-26 2012-07-26 Inhibitors of the renal outer medullary potassium channel
US201261691390P 2012-08-21 2012-08-21
US201361759040P 2013-01-31 2013-01-31
PCT/US2013/052079 WO2014018764A1 (en) 2012-07-26 2013-07-25 Spiro - fused piperidine derivatives for use as inhibitors of the renal outer medullary potassium channel

Publications (2)

Publication Number Publication Date
MX2015001115A MX2015001115A (es) 2015-04-08
MX365986B true MX365986B (es) 2019-06-20

Family

ID=48916271

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015001115A MX365986B (es) 2012-07-26 2013-07-25 Derivativos de piperidina fusionados con espiro para usarse como inhibidores del canal de potasio medular externo renal.

Country Status (14)

Country Link
US (2) US8952166B2 (es)
EP (1) EP2877471B1 (es)
JP (1) JP6166783B2 (es)
KR (1) KR20150036142A (es)
CN (1) CN104540826B (es)
AR (1) AR092031A1 (es)
AU (1) AU2013295722B2 (es)
BR (1) BR112015001419A8 (es)
CA (1) CA2876508A1 (es)
ES (1) ES2606016T3 (es)
MX (1) MX365986B (es)
RU (1) RU2642066C2 (es)
TW (1) TW201410675A (es)
WO (1) WO2014018764A1 (es)

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WO2012058134A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9062070B2 (en) 2011-08-19 2015-06-23 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9527830B2 (en) 2011-09-16 2016-12-27 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2771004B1 (en) 2011-10-25 2016-05-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US8999990B2 (en) 2011-10-25 2015-04-07 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2773206B1 (en) 2011-10-31 2018-02-21 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2773351B1 (en) 2011-10-31 2017-08-23 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9139585B2 (en) 2011-10-31 2015-09-22 Merck Sharp & Dohme Corp. Inhibitors of the Renal Outer Medullary Potassium channel
EP2790511B1 (en) 2011-12-16 2016-09-14 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2014085210A1 (en) 2012-11-29 2014-06-05 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2934533B1 (en) 2012-12-19 2017-11-15 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9604998B2 (en) 2013-02-18 2017-03-28 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2014150132A1 (en) * 2013-03-15 2014-09-25 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9751881B2 (en) 2013-07-31 2017-09-05 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP3063142B1 (en) 2013-10-31 2019-01-30 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2015103756A1 (en) 2014-01-09 2015-07-16 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
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WO2016069428A1 (en) * 2014-10-31 2016-05-06 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
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WO2016122994A1 (en) * 2015-01-29 2016-08-04 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2016127358A1 (en) * 2015-02-12 2016-08-18 Merck Sharp & Dohme Corp. Inhibitors of renal outer medullary potassium channel
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MA43677A (fr) 2016-02-25 2018-11-28 Asceneuron Sa Inhibiteurs de glycosidases
AU2017252546B2 (en) 2016-04-20 2021-07-29 Bristol-Myers Squibb Company Substituted bicyclic heterocyclic compounds
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CN109906218B (zh) 2016-08-01 2023-01-17 阿普廷伊克斯股份有限公司 螺-内酰胺nmda受体调节剂及其用途
JP2019527232A (ja) 2016-08-01 2019-09-26 アプティニックス インコーポレイテッド スピロ−ラクタムnmda修飾因子及びこれを用いた方法
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CN106432214B (zh) * 2016-08-09 2019-05-07 成都拿盛科技有限公司 一种制备romk通道抑制剂中间体的方法
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CN107569495A (zh) * 2017-08-10 2018-01-12 新疆医科大学 依普利酮对慢性心力衰竭患者辅助性t细胞活化/增殖的抑制作用
KR20200096802A (ko) * 2017-12-06 2020-08-13 지앙수 헨그루이 메디슨 컴퍼니 리미티드 신장 외수질 칼륨 채널 억제제인 결정 형태 및 이의 제조 방법
CN109879863B (zh) * 2017-12-06 2020-10-20 江苏恒瑞医药股份有限公司 一种肾外髓质分泌钾通道抑制剂的晶型及其制备方法
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MX2015001115A (es) 2015-04-08
JP6166783B2 (ja) 2017-07-19
US20150099729A1 (en) 2015-04-09
CN104540826B (zh) 2018-04-20
BR112015001419A8 (pt) 2019-07-30
EP2877471B1 (en) 2016-11-02
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AU2013295722A1 (en) 2015-01-15
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AR092031A1 (es) 2015-03-18
WO2014018764A1 (en) 2014-01-30
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US8952166B2 (en) 2015-02-10
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BR112015001419A2 (pt) 2017-07-04

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