CA3143965A1 - Polymorphic forms of (r)-4-(1-((3-(difluoromethyl)-1-methyl-1h-pyrazol-4-yl)sulfonyl)-1-fluoroethyl)-n-(isoxazol-3-yl)piperidine-1-carboxamide - Google Patents

Polymorphic forms of (r)-4-(1-((3-(difluoromethyl)-1-methyl-1h-pyrazol-4-yl)sulfonyl)-1-fluoroethyl)-n-(isoxazol-3-yl)piperidine-1-carboxamide Download PDF

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Publication number
CA3143965A1
CA3143965A1 CA3143965A CA3143965A CA3143965A1 CA 3143965 A1 CA3143965 A1 CA 3143965A1 CA 3143965 A CA3143965 A CA 3143965A CA 3143965 A CA3143965 A CA 3143965A CA 3143965 A1 CA3143965 A1 CA 3143965A1
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Prior art keywords
polymorph
composition
degrees
theta
diffraction pattern
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Pending
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CA3143965A
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English (en)
French (fr)
Inventor
Min Zhong
Olivier Monnier
Jean-Philippe JELIN
Richard DUVOUX
Jean Alie
Philippe Ochsenbein
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Myokardia Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (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)
CA3143965A 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 Pending CA3143965A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962874855P 2019-07-16 2019-07-16
US62/874,855 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
CA3143965A1 true CA3143965A1 (en) 2021-01-21

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CA3143965A Pending CA3143965A1 (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

Country Status (15)

Country Link
US (3) US20210053939A1 (cg-RX-API-DMAC10.html)
EP (1) EP3999504A1 (cg-RX-API-DMAC10.html)
JP (2) JP2022540678A (cg-RX-API-DMAC10.html)
KR (1) KR20220035176A (cg-RX-API-DMAC10.html)
CN (1) CN114127061A (cg-RX-API-DMAC10.html)
AU (1) AU2020315605B2 (cg-RX-API-DMAC10.html)
BR (1) BR112022000474A2 (cg-RX-API-DMAC10.html)
CA (1) CA3143965A1 (cg-RX-API-DMAC10.html)
CL (1) CL2022000050A1 (cg-RX-API-DMAC10.html)
CO (1) CO2022000117A2 (cg-RX-API-DMAC10.html)
IL (1) IL289817A (cg-RX-API-DMAC10.html)
MX (1) MX2022000606A (cg-RX-API-DMAC10.html)
PE (1) PE20220645A1 (cg-RX-API-DMAC10.html)
TW (1) TWI921306B (cg-RX-API-DMAC10.html)
WO (1) WO2021011586A1 (cg-RX-API-DMAC10.html)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116082326B (zh) * 2022-12-16 2024-12-27 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
WO2025244956A1 (en) 2024-05-20 2025-11-27 MyoKardia, Inc. Methods of manufacturing danicamtiv

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BR0007784A (pt) 1999-01-27 2002-02-05 American Cyanamid Co Composto, método para inibir mudanças patológicas mediadas pela enzima que converte o tnf-alfa (tace) em um mamìfero, composição farmacêutica, e, processo para preparar um composto
WO2005117882A2 (en) 2004-04-20 2005-12-15 Incyte Corporation Hydroxamic acid derivatives as metalloprotease inhibitors
US7507735B2 (en) 2004-06-17 2009-03-24 Cytokinetics, Inc. Compounds, compositions and methods
WO2006074025A1 (en) 2004-12-30 2006-07-13 Janssen Pharmaceutica N.V. Piperazinyl and piperidinyl ureas as modulators of fatty acid amide hydrolase
EP1866285A1 (en) 2005-03-03 2007-12-19 F. Hoffmann-Roche AG 1-sulfonyl-piperdine-3-carboxylic acid amide derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase for the treatment of type ii diabetes mellitus
WO2008120759A1 (ja) 2007-03-30 2008-10-09 Japan Tobacco Inc. ウレア化合物およびその用途
ES2442003T3 (es) 2007-06-20 2014-02-07 Mitsubishi Tanabe Pharma Corporation Nuevo derivado de sulfonamida de ácido malónico y uso farmacéutico del mismo
WO2009011850A2 (en) 2007-07-16 2009-01-22 Abbott Laboratories Novel therapeutic compounds
ES2499018T3 (es) 2007-09-20 2014-09-26 Irm Llc Compuestos y composiciones como moduladores de la actividad de GPR119
MX2010003621A (es) 2007-10-01 2010-04-14 Hoffmann La Roche N-heterociclil biaril carboxamidas como antagonistas del receptor ccr.
WO2009047161A1 (en) 2007-10-09 2009-04-16 F. Hoffmann-La Roche Ag Chiral cis-imidazolines
SG188117A1 (en) 2008-06-19 2013-03-28 Takeda Pharmaceutical Heterocyclic compound and use thereof
US8324178B2 (en) 2008-10-31 2012-12-04 The Regents Of The University Of California Method of treatment using alpha-1-adrenergic agonist compounds
JP5329646B2 (ja) 2009-04-01 2013-10-30 パナソニック株式会社 デジタル周波数／位相ロックドループ
WO2011059021A1 (ja) 2009-11-11 2011-05-19 大日本住友製薬株式会社 ８－アザビシクロ［３．２．１］オクタン－８－カルボキサミド誘導体
WO2015005305A1 (ja) 2013-07-09 2015-01-15 小野薬品工業株式会社 Ａｌｘｒ作動化合物
HUE037134T2 (hu) 2013-08-07 2018-08-28 Merck Patent Gmbh Piperidin-karbamid-származékok
WO2015112806A2 (en) 2014-01-24 2015-07-30 Tp Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
SG11201705928XA (en) * 2015-01-22 2017-08-30 Myokardia Inc 4-methylsulfonyl-substituted piperidine urea compounds for the treatment of dilated cardiomyopathy (dcm)
SG11202112723PA (en) 2019-05-19 2021-12-30 Myokardia Inc 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

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Publication number Publication date
US12459919B2 (en) 2025-11-04
IL289817A (en) 2022-03-01
AU2020315605A1 (en) 2022-03-03
CN114127061A (zh) 2022-03-01
JP2025148397A (ja) 2025-10-07
US20260193230A1 (en) 2026-07-09
MX2022000606A (es) 2022-03-11
US20210053939A1 (en) 2021-02-25
TWI921306B (zh) 2026-04-11
CO2022000117A2 (es) 2022-01-17
TW202116765A (zh) 2021-05-01
US20220289709A1 (en) 2022-09-15
EP3999504A1 (en) 2022-05-25
AU2020315605B2 (en) 2026-05-28
KR20220035176A (ko) 2022-03-21
WO2021011586A1 (en) 2021-01-21
PE20220645A1 (es) 2022-04-28
BR112022000474A2 (pt) 2022-05-17
CL2022000050A1 (es) 2022-10-14
JP2022540678A (ja) 2022-09-16

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