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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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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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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ID=71895284

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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 (14)

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

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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US6358980B1 (en) 1999-01-27 2002-03-19 American Cyanamid Company Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase/tace inhibitors
US20050250789A1 (en) 2004-04-20 2005-11-10 Burns David M Hydroxamic acid derivatives as metalloprotease inhibitors
ES2522579T3 (es) 2004-06-17 2014-11-17 Cytokinetics, Inc. Compuestos, composiciones y métodos
NZ590148A (en) 2004-12-30 2012-04-27 Janssen Pharmaceutica Nv 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
RU2462454C2 (ru) 2007-06-20 2012-09-27 Мицубиси Танабе Фарма Корпорейшн Новое сульфонамидное производное малоновой кислоты и его фармацевтическое применение
WO2009011850A2 (en) 2007-07-16 2009-01-22 Abbott Laboratories Novel therapeutic compounds
BRPI0817211A2 (pt) 2007-09-20 2017-05-16 Irm Llc composto composições como moduladores da atividade de gpr119
RU2010116821A (ru) 2007-10-01 2011-11-10 Ф.Хоффманн-Ля Аг (Ch) N-гетероциклические биарильные карбоксамиды в качестве антагонистов рецептора ccr
RU2487127C2 (ru) 2007-10-09 2013-07-10 Ф.Хоффманн-Ля Рош Аг Хиральные цис-имидазолины
NZ600238A (en) 2008-06-19 2014-04-30 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
WO2010113377A1 (ja) 2009-04-01 2010-10-07 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
TWI472331B (zh) 2009-11-11 2015-02-11 Sumitomo Dainippon Pharma Co Ltd ８－氮雙環〔３‧２‧１〕辛烷－８－羧醯胺衍生物
US9771357B2 (en) 2013-07-09 2017-09-26 Ono Pharmaceutical Co., Ltd. ALXR agonist compound
KR102249564B1 (ko) 2013-08-07 2021-05-07 메르크 파텐트 게엠베하 피페리딘 우레아 유도체
ES2933350T3 (es) 2014-01-24 2023-02-06 Turning Point Therapeutics Inc Macrociclos de diarilo como moduladores de proteína quinasas
EP4234017B1 (en) * 2015-01-22 2026-04-15 MyoKardia, Inc. Preparation of 4-methylsulfonyl-substituted piperidine urea compounds useful for the treatment of cardiac disorders such as dilated cardiomyopathy (dcm)
KR20220009440A (ko) 2019-05-19 2022-01-24 미요카디아, 인크. 화합물 (r)-4-(1-((3-(디플루오로메틸)-1-메틸-1h-피라졸-4-일)술포닐)-1-플루오로에틸)-n-(이속사졸-3-일)피페리딘-1-카르복스아미드를 사용한 수축기 기능장애 및 감소된 박출 계수를 가진 심부전의 치료

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

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