AU2016220348B2 - (2R,4R)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid - Google Patents

(2R,4R)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid Download PDF

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Publication number
AU2016220348B2
AU2016220348B2 AU2016220348A AU2016220348A AU2016220348B2 AU 2016220348 B2 AU2016220348 B2 AU 2016220348B2 AU 2016220348 A AU2016220348 A AU 2016220348A AU 2016220348 A AU2016220348 A AU 2016220348A AU 2016220348 B2 AU2016220348 B2 AU 2016220348B2
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Australia
Prior art keywords
compound
crystalline form
administered
acid
chloro
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AU2016220348A
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AU2016220348A1 (en
Inventor
Anne-Marie Beausoleil
Erik FENSTER
Melissa Fleury
Adam D. Hughes
Miroslav Rapta
Venkat R. Thalladi
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Theravance Biopharma R&D IP LLC
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Theravance Biopharma R&D IP LLC
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • A61K9/4825—Proteins, e.g. gelatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C30—CRYSTAL GROWTH
    • C30B—SINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B29/00—Single crystals or homogeneous polycrystalline material with defined structure characterised by the material or by their shape
    • C30B29/54—Organic compounds
    • C—CHEMISTRY; METALLURGY
    • C30—CRYSTAL GROWTH
    • C30B—SINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B7/00—Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions
    • C30B7/14—Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions the crystallising materials being formed by chemical reactions in the solution
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Materials Engineering (AREA)
  • Metallurgy (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicinal Preparation (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU2016220348A 2015-02-19 2016-02-12 (2R,4R)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid Ceased AU2016220348B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562118067P 2015-02-19 2015-02-19
US62/118,067 2015-02-19
PCT/US2016/017699 WO2016133803A1 (en) 2015-02-19 2016-02-12 (2r,4r)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid

Publications (2)

Publication Number Publication Date
AU2016220348A1 AU2016220348A1 (en) 2017-08-17
AU2016220348B2 true AU2016220348B2 (en) 2019-10-17

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AU2016220348A Ceased AU2016220348B2 (en) 2015-02-19 2016-02-12 (2R,4R)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid

Country Status (29)

Country Link
US (6) US9533962B2 (enExample)
EP (1) EP3259255B1 (enExample)
JP (1) JP6714009B2 (enExample)
KR (1) KR102573351B1 (enExample)
CN (1) CN107250119B (enExample)
AU (1) AU2016220348B2 (enExample)
BR (1) BR112017017783A2 (enExample)
CA (1) CA2975269C (enExample)
CO (1) CO2017008426A2 (enExample)
CY (1) CY1123728T1 (enExample)
DK (1) DK3259255T3 (enExample)
ES (1) ES2857101T3 (enExample)
HR (1) HRP20210040T1 (enExample)
HU (1) HUE052732T2 (enExample)
IL (1) IL253759B (enExample)
LT (1) LT3259255T (enExample)
MX (1) MX370065B (enExample)
MY (1) MY191183A (enExample)
PH (1) PH12017501444A1 (enExample)
PL (1) PL3259255T3 (enExample)
PT (1) PT3259255T (enExample)
RS (1) RS61325B1 (enExample)
RU (1) RU2715241C2 (enExample)
SG (1) SG11201706662YA (enExample)
SI (1) SI3259255T1 (enExample)
SM (1) SMT202100028T1 (enExample)
TW (1) TWI707846B (enExample)
WO (1) WO2016133803A1 (enExample)
ZA (1) ZA201705487B (enExample)

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KR102238177B1 (ko) 2017-09-15 2021-04-07 주식회사 엘지화학 전지셀 및 전극 리드 제조방법
UY38072A (es) 2018-02-07 2019-10-01 Novartis Ag Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos
CA3145579A1 (en) * 2019-07-03 2021-01-07 Merck Patent Gmbh Process for manufacturing (s)-3-hydroxy-1-(1h-indol-5-yl)-2-oxo-pyrrolidine-3-carboxylic acid 3,5-difluoro-benzylamide

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US20100305145A1 (en) * 2009-05-28 2010-12-02 Gary Mark Coppola Substituted Aminobutyric Derivatives as Neprilysin Inhibitors
US8372984B2 (en) * 2009-07-22 2013-02-12 Theravance, Inc. Dual-acting oxazole antihypertensive agents
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US9872855B2 (en) * 2015-02-19 2018-01-23 Theravance Biopharma R&D Ip, Llc (2R,4R)-5-(5′-Chloro-2′-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid

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US20170196841A1 (en) 2017-07-13
US9533962B2 (en) 2017-01-03
NZ734623A (en) 2021-01-29
IL253759B (en) 2020-10-29
CO2017008426A2 (es) 2017-11-10
US11033533B2 (en) 2021-06-15
RU2017132430A3 (enExample) 2019-08-12
TW201638074A (zh) 2016-11-01
CA2975269A1 (en) 2016-08-25
US20190269659A1 (en) 2019-09-05
US20210401808A1 (en) 2021-12-30
HK1245772A1 (zh) 2018-08-31
CY1123728T1 (el) 2022-05-27
US10548879B2 (en) 2020-02-04
US20200281900A1 (en) 2020-09-10
LT3259255T (lt) 2021-04-26
RS61325B1 (sr) 2021-02-26
AU2016220348A1 (en) 2017-08-17
PL3259255T3 (pl) 2021-07-26
CA2975269C (en) 2023-09-19
IL253759A0 (en) 2017-09-28
US20180228774A1 (en) 2018-08-16
US10172834B2 (en) 2019-01-08
HRP20210040T1 (hr) 2021-04-02
PT3259255T (pt) 2021-01-26
BR112017017783A2 (pt) 2018-07-17
TWI707846B (zh) 2020-10-21
US9872855B2 (en) 2018-01-23
PH12017501444A1 (en) 2018-01-15
WO2016133803A1 (en) 2016-08-25
SMT202100028T1 (it) 2021-03-15
EP3259255B1 (en) 2020-10-21
MY191183A (en) 2022-06-04
DK3259255T3 (da) 2021-01-18
MX2017010666A (es) 2017-11-16
ES2857101T3 (es) 2021-09-28
JP2018507207A (ja) 2018-03-15
RU2017132430A (ru) 2019-03-19
CN107250119B (zh) 2020-09-22
SG11201706662YA (en) 2017-09-28
CN107250119A (zh) 2017-10-13
US11642332B2 (en) 2023-05-09
US20160244416A1 (en) 2016-08-25
RU2715241C2 (ru) 2020-02-26
KR102573351B1 (ko) 2023-09-01
KR20170118855A (ko) 2017-10-25
EP3259255A1 (en) 2017-12-27
ZA201705487B (en) 2018-05-30
MX370065B (es) 2019-11-29
SI3259255T1 (sl) 2021-04-30
HUE052732T2 (hu) 2021-05-28
JP6714009B2 (ja) 2020-06-24

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