PE20220645A1 - Formas polimorficas de (r)-4- (1-((3- (difluorometil)-1-metil-1h- pirazol-4-il)sulfonil) -1- fluoroetil)-n-(isoxazol-3-il)piperidina -1- carboxamida - Google Patents

Formas polimorficas de (r)-4- (1-((3- (difluorometil)-1-metil-1h- pirazol-4-il)sulfonil) -1- fluoroetil)-n-(isoxazol-3-il)piperidina -1- carboxamida

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Publication number
PE20220645A1
PE20220645A1 PE2022000049A PE2022000049A PE20220645A1 PE 20220645 A1 PE20220645 A1 PE 20220645A1 PE 2022000049 A PE2022000049 A PE 2022000049A PE 2022000049 A PE2022000049 A PE 2022000049A PE 20220645 A1 PE20220645 A1 PE 20220645A1
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PE
Peru
Prior art keywords
fluoroethyl
pyrazol
carboxamide
piperidine
methyl
Prior art date
Application number
PE2022000049A
Other languages
English (en)
Inventor
Min Zhong
Olivier Monnier
Jean-Phillippe Jelin
Richard Duvoux
Jean Alie
Phillippe Ochsenbein
Original Assignee
Myokardia Inc
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 Myokardia Inc filed Critical Myokardia Inc
Publication of PE20220645A1 publication Critical patent/PE20220645A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61P9/08Vasodilators for multiple indications
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Cardiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invencion proporciona nuevos polimorfos de (R)-4-(1-((3- (difluorometil)-1-metil-1H-pirazol-4-il)sulfonil)-1-fluoroetil)-N-(isoxazol-3 -il) piperidina-1- carboxamida (I-491) que son utiles para el tratamiento de trastornos cardiacos que incluyen disfuncion sistolica, miocardiopatia dilatada (DCM), insuficiencia cardiaca con fraccion de eyeccion reservada (HFrEF) y afecciones asociadas con el lado izquierdo y/o disfuncion sistolica del ventriculo derecho o reserva sistolica. Se describe la sintesis y caracterizacion de los polimorfos, asi como los metodos para tratar la disfuncion sistolica, DCM, HFrEF y otras formas de enfermedad cardiaca.
PE2022000049A 2019-07-16 2020-07-15 Formas polimorficas de (r)-4- (1-((3- (difluorometil)-1-metil-1h- pirazol-4-il)sulfonil) -1- fluoroetil)-n-(isoxazol-3-il)piperidina -1- carboxamida PE20220645A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962874855P 2019-07-16 2019-07-16
PCT/US2020/042028 WO2021011586A1 (en) 2019-07-16 2020-07-15 Polymorphic forms of (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
PE20220645A1 true PE20220645A1 (es) 2022-04-28

Family

ID=71895284

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000049A PE20220645A1 (es) 2019-07-16 2020-07-15 Formas polimorficas de (r)-4- (1-((3- (difluorometil)-1-metil-1h- pirazol-4-il)sulfonil) -1- fluoroetil)-n-(isoxazol-3-il)piperidina -1- carboxamida

Country Status (15)

Country Link
US (2) US20210053939A1 (es)
EP (1) EP3999504A1 (es)
JP (1) JP2022540678A (es)
KR (1) KR20220035176A (es)
CN (1) CN114127061A (es)
AU (1) AU2020315605A1 (es)
BR (1) BR112022000474A2 (es)
CA (1) CA3143965A1 (es)
CL (1) CL2022000050A1 (es)
CO (1) CO2022000117A2 (es)
IL (1) IL289817A (es)
MX (1) MX2022000606A (es)
PE (1) PE20220645A1 (es)
TW (1) TW202116765A (es)
WO (1) WO2021011586A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN117865941B (zh) * 2024-03-13 2024-06-28 上海方予健康医药科技有限公司 取代哌啶化合物及其制备方法和应用

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111393414B (zh) * 2015-01-22 2024-05-07 迈奥卡迪亚公司 用于治疗扩张性心肌病(dcm)的4-甲基磺酰基取代的哌啶脲化合物

Also Published As

Publication number Publication date
CN114127061A (zh) 2022-03-01
CO2022000117A2 (es) 2022-01-17
CA3143965A1 (en) 2021-01-21
EP3999504A1 (en) 2022-05-25
AU2020315605A1 (en) 2022-03-03
US20220289709A1 (en) 2022-09-15
IL289817A (en) 2022-03-01
TW202116765A (zh) 2021-05-01
MX2022000606A (es) 2022-03-11
JP2022540678A (ja) 2022-09-16
KR20220035176A (ko) 2022-03-21
WO2021011586A1 (en) 2021-01-21
BR112022000474A2 (pt) 2022-05-17
CL2022000050A1 (es) 2022-10-14
US20210053939A1 (en) 2021-02-25

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