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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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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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)
  • 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)
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 (14)

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

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
JP5080970B2 (ja) 2004-06-17 2012-11-21 サイトキネティクス・インコーポレーテッド 心疾患を治療するための置換尿素誘導体
AR055831A1 (es) 2004-12-30 2007-09-12 Janssen Pharmaceutica Nv Pepirazinilureas y piperidinilureas como moduladores de hidrolasa de amida de acidos grasos
KR100979577B1 (ko) 2005-03-03 2010-09-01 에프. 호프만-라 로슈 아게 2형 진성 당뇨병의 치료를 위한11-베타-하이드록시스테로이드 탈수소효소의 억제제로서1-설폰일-피페리딘-3-카복실산 아마이드 유도체
WO2008120759A1 (ja) 2007-03-30 2008-10-09 Japan Tobacco Inc. ウレア化合物およびその用途
US8461209B2 (en) 2007-06-20 2013-06-11 Mitsubishi Tanabe Pharma Corporation Malonic acid sulfonamide derivative and pharmaceutical use thereof
US20090069288A1 (en) 2007-07-16 2009-03-12 Breinlinger Eric C Novel therapeutic compounds
RU2443699C2 (ru) 2007-09-20 2012-02-27 Айрм Ллк Соединения и композиции в качестве модуляторов активности gpr119
CN101801952A (zh) 2007-10-01 2010-08-11 弗·哈夫曼-拉罗切有限公司 用作ccr受体拮抗剂的n-杂环联芳基甲酰胺类化合物
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CN102596949B (zh) 2009-11-11 2015-08-19 大日本住友制药株式会社 8-氮杂双环[3.2.1]辛烷-8-甲酰胺衍生物
WO2015005305A1 (ja) 2013-07-09 2015-01-15 小野薬品工業株式会社 Ａｌｘｒ作動化合物
NZ717552A (en) 2013-08-07 2021-07-30 Merck Patent Gmbh Piperidine urea derivatives
PL3636649T3 (pl) 2014-01-24 2024-05-06 Turning Point Therapeutics, Inc. Diaryle makrocykliczne jako modulatory kinaz białkowych
IL295547A (en) 2015-01-22 2022-10-01 Myokardia Inc Piperidine-4-methylsulfonyl-modified urea compounds for the treatment of dilated cardiomyopathy (dcm)
WO2020236736A1 (en) 2019-05-19 2020-11-26 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
US20210053939A1 (en) 2021-02-25
JP2025148397A (ja) 2025-10-07
JP2022540678A (ja) 2022-09-16
US20220289709A1 (en) 2022-09-15
PE20220645A1 (es) 2022-04-28
IL289817A (en) 2022-03-01
CO2022000117A2 (es) 2022-01-17
US12459919B2 (en) 2025-11-04
BR112022000474A2 (pt) 2022-05-17
MX2022000606A (es) 2022-03-11
CN114127061A (zh) 2022-03-01
TW202116765A (zh) 2021-05-01
AU2020315605A1 (en) 2022-03-03
CL2022000050A1 (es) 2022-10-14
EP3999504A1 (en) 2022-05-25
KR20220035176A (ko) 2022-03-21
WO2021011586A1 (en) 2021-01-21

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