PE20220426A1 - Tratamiento de la disfuncion sistolica e insuficiencia cardiaca con fraccion de eyeccion reducida con el compuesto (r) -4-(1-((3-(difluorometil) -1-metil-1h-pirazol-4-il) sulfonil) -1-fluoroetil) -n-(isoxazol-3-il) piperidin-1-carboxamida - Google Patents

Tratamiento de la disfuncion sistolica e insuficiencia cardiaca con fraccion de eyeccion reducida con el compuesto (r) -4-(1-((3-(difluorometil) -1-metil-1h-pirazol-4-il) sulfonil) -1-fluoroetil) -n-(isoxazol-3-il) piperidin-1-carboxamida

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Publication number
PE20220426A1
PE20220426A1 PE2021001920A PE2021001920A PE20220426A1 PE 20220426 A1 PE20220426 A1 PE 20220426A1 PE 2021001920 A PE2021001920 A PE 2021001920A PE 2021001920 A PE2021001920 A PE 2021001920A PE 20220426 A1 PE20220426 A1 PE 20220426A1
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PE
Peru
Prior art keywords
compound
fluoroethyl
pyrazol
carboxamide
methyl
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PE2021001920A
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English (en)
Inventor
Jean-Francois Tamby
Chun Yang
Timothy Carlson
Original Assignee
Myokardia Inc
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Publication date
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Publication of PE20220426A1 publication Critical patent/PE20220426A1/es

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    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • 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
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

Esta referido a un metodo para tratar la disfuncion sistolica, el cual comprende la administracion oral al paciente del Compuesto I en una cantidad diaria total de 10-350 mg, en donde el Compuesto I es (R)-4-(1-((3-(difluorometil)-1-metil-1H-pirazol-4-il)sulfonil)-1- fluoroetil)-N-(isoxazol-3-il)piperidina-1-carboxamida. Este metodo se emplea en el tratamiento de un sindrome o trastorno seleccionado del grupo que consiste en insuficiencia cardiaca, miocardiopatia, choque cardiogenico, una afeccion que se beneficia del soporte inotropico despues de una cirugia cardiaca, miocarditis, aterosclerosis, aldosteronismo secundario, infarto de miocardio, valvulopatia, hipertension sistemica, hipertension pulmonar o hipertension arterial pulmonar, remodelacion vascular perjudicial, edema pulmonar e insuficiencia respiratoria.
PE2021001920A 2019-05-19 2020-05-18 Tratamiento de la disfuncion sistolica e insuficiencia cardiaca con fraccion de eyeccion reducida con el compuesto (r) -4-(1-((3-(difluorometil) -1-metil-1h-pirazol-4-il) sulfonil) -1-fluoroetil) -n-(isoxazol-3-il) piperidin-1-carboxamida PE20220426A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962849936P 2019-05-19 2019-05-19
US201962852739P 2019-05-24 2019-05-24
PCT/US2020/033438 WO2020236736A1 (en) 2019-05-19 2020-05-18 Treatment of systolic dysfunction and heart failure with reduced ejection fraction with the compound(r)-4-(1-((3-(difluoromethyl)-1-methyl-1h-pyrazol-4-yl)sulfonyl)-1-fluoroethyl)-n-(isoxazol-3-yl)piperidine-1-carboxamide

Publications (1)

Publication Number Publication Date
PE20220426A1 true PE20220426A1 (es) 2022-03-29

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PE2021001920A PE20220426A1 (es) 2019-05-19 2020-05-18 Tratamiento de la disfuncion sistolica e insuficiencia cardiaca con fraccion de eyeccion reducida con el compuesto (r) -4-(1-((3-(difluorometil) -1-metil-1h-pirazol-4-il) sulfonil) -1-fluoroetil) -n-(isoxazol-3-il) piperidin-1-carboxamida

Country Status (16)

Country Link
US (1) US20220265629A1 (es)
EP (1) EP3972597A1 (es)
JP (1) JP2022535195A (es)
KR (1) KR20220009440A (es)
CN (1) CN114173782A (es)
AU (1) AU2020279710A1 (es)
BR (1) BR112021023074A2 (es)
CA (1) CA3138080A1 (es)
CL (1) CL2021003045A1 (es)
CO (1) CO2021015505A2 (es)
IL (1) IL288051A (es)
MX (1) MX2021014109A (es)
PE (1) PE20220426A1 (es)
SG (1) SG11202112723PA (es)
TW (1) TW202110449A (es)
WO (1) WO2020236736A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7316449B2 (ja) * 2019-09-20 2023-07-27 シェンヅェン サルブリス ファーマシューティカルズ カンパニー リミテッド 心不全治療におけるアンジオテンシンii受容体アンタゴニスト代謝産物とnep阻害剤との複合体の使用
AU2021293817A1 (en) * 2020-06-15 2023-01-19 MyoKardia, Inc. Treatment of atrial dysfunction
WO2023102452A1 (en) * 2021-12-02 2023-06-08 Tenax Therapeutics, Inc. Use of a combination of levosimendan and an sglt-2 inhibitor to treat heart failure
CN116082326A (zh) * 2022-12-16 2023-05-09 药康众拓(江苏)医药科技有限公司北京分公司 一种氘代吡唑磺酰甲基-哌啶异噁唑脲类化合物及其用途

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2403533A (en) * 2003-06-30 2005-01-05 Orion Corp Atrial natriuretic peptide and brain natriuretic peptide and assays and uses thereof
US20050250789A1 (en) * 2004-04-20 2005-11-10 Burns David M Hydroxamic acid derivatives as metalloprotease inhibitors
US8324178B2 (en) * 2008-10-31 2012-12-04 The Regents Of The University Of California Method of treatment using alpha-1-adrenergic agonist compounds
LT3247707T (lt) * 2015-01-22 2023-08-25 MyoKardia, Inc. 4-metilsulfonilu pakeistieji piperidino karbamido junginiai, naudotini širdies sutrikimų, tokių kaip dilatacinė kardiomiopatija (dcm), gydymui

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WO2020236736A1 (en) 2020-11-26
CL2021003045A1 (es) 2022-07-08
CN114173782A (zh) 2022-03-11
CA3138080A1 (en) 2020-11-26
TW202110449A (zh) 2021-03-16
EP3972597A1 (en) 2022-03-30
IL288051A (en) 2022-01-01
MX2021014109A (es) 2021-12-10
AU2020279710A1 (en) 2021-12-23
CO2021015505A2 (es) 2021-12-10
US20220265629A1 (en) 2022-08-25
BR112021023074A2 (pt) 2022-03-29
SG11202112723PA (en) 2021-12-30
JP2022535195A (ja) 2022-08-05
KR20220009440A (ko) 2022-01-24

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