CA3015505C - Crystalline (2s,4r)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof - Google Patents

Crystalline (2s,4r)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof Download PDF

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Publication number
CA3015505C
CA3015505C CA3015505A CA3015505A CA3015505C CA 3015505 C CA3015505 C CA 3015505C CA 3015505 A CA3015505 A CA 3015505A CA 3015505 A CA3015505 A CA 3015505A CA 3015505 C CA3015505 C CA 3015505C
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CA
Canada
Prior art keywords
compound
crystalline form
administered
hypertension
acid
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CA3015505A
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English (en)
French (fr)
Other versions
CA3015505A1 (en
Inventor
Adam D. Hughes
Melissa Fleury
Miroslav Rapta
Venkat R. Thalladi
Gene Timothy Fass
Michael SIMEONE
R. Michael BALDWIN
David L. BOURDET
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Theravance Biopharma R&D IP LLC
Original Assignee
Theravance Biopharma R&D IP LLC
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=58387911&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA3015505(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Theravance Biopharma R&D IP LLC filed Critical Theravance Biopharma R&D IP LLC
Publication of CA3015505A1 publication Critical patent/CA3015505A1/en
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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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CA3015505A 2016-03-08 2017-03-07 Crystalline (2s,4r)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof Active CA3015505C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662305393P 2016-03-08 2016-03-08
US62/305,393 2016-03-08
US201662346336P 2016-06-06 2016-06-06
US62/346,336 2016-06-06
PCT/US2017/021172 WO2017156009A1 (en) 2016-03-08 2017-03-07 Crystalline(2s,4r)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof

Publications (2)

Publication Number Publication Date
CA3015505A1 CA3015505A1 (en) 2017-09-14
CA3015505C true CA3015505C (en) 2024-03-05

Family

ID=58387911

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3015505A Active CA3015505C (en) 2016-03-08 2017-03-07 Crystalline (2s,4r)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof

Country Status (30)

Country Link
US (6) US10100021B2 (enExample)
EP (1) EP3408260B1 (enExample)
JP (2) JP7306828B2 (enExample)
KR (2) KR20220035991A (enExample)
CN (1) CN108779084A (enExample)
AU (1) AU2017229466C1 (enExample)
CA (1) CA3015505C (enExample)
CL (1) CL2018002539A1 (enExample)
CO (1) CO2018010568A2 (enExample)
CY (1) CY1124397T1 (enExample)
DK (1) DK3408260T3 (enExample)
ES (1) ES2880123T3 (enExample)
HR (1) HRP20211169T1 (enExample)
HU (1) HUE055546T2 (enExample)
IL (1) IL261244B (enExample)
LT (1) LT3408260T (enExample)
MX (1) MX377177B (enExample)
MY (1) MY198185A (enExample)
PH (1) PH12018501876A1 (enExample)
PL (1) PL3408260T3 (enExample)
PT (1) PT3408260T (enExample)
RS (1) RS62172B1 (enExample)
RU (1) RU2756223C2 (enExample)
SA (1) SA518392325B1 (enExample)
SG (1) SG11201807591VA (enExample)
SI (1) SI3408260T1 (enExample)
SM (1) SMT202100434T1 (enExample)
TW (1) TWI731943B (enExample)
WO (1) WO2017156009A1 (enExample)
ZA (1) ZA201805840B (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
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TWI731943B (zh) 2016-03-08 2021-07-01 美商施萬生物製藥研發Ｉｐ有限責任公司 結晶型（2s，4r）－5－（5’－氯－2’－氟－［1，1’－聯苯］－4－基）－2－（乙氧基甲基）－4－（3－羥基異㗁唑－5－甲醯胺基）－2－甲基戊酸及其用途
WO2021052441A1 (zh) 2019-09-20 2021-03-25 深圳信立泰药业股份有限公司 血管紧张素ii受体拮抗剂代谢产物与nep抑制剂的复合物治疗心衰的用途
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Also Published As

Publication number Publication date
US10100021B2 (en) 2018-10-16
US20240327360A1 (en) 2024-10-03
CL2018002539A1 (es) 2018-10-26
JP7306828B2 (ja) 2023-07-11
HRP20211169T1 (hr) 2021-11-12
US11718591B2 (en) 2023-08-08
US10752599B2 (en) 2020-08-25
IL261244A (en) 2018-10-31
EP3408260A1 (en) 2018-12-05
CN108779084A (zh) 2018-11-09
WO2017156009A1 (en) 2017-09-14
ZA201805840B (en) 2019-07-31
BR112018068170A2 (pt) 2019-01-29
EP3408260B1 (en) 2021-05-05
US11230536B2 (en) 2022-01-25
SA518392325B1 (ar) 2022-08-03
RU2018135072A3 (enExample) 2020-10-15
MX377177B (es) 2025-03-07
IL261244B (en) 2022-02-01
PH12018501876A1 (en) 2019-01-28
US20210061776A1 (en) 2021-03-04
TWI731943B (zh) 2021-07-01
ES2880123T3 (es) 2021-11-23
PT3408260T (pt) 2021-07-23
US20200157061A1 (en) 2020-05-21
JP2022017433A (ja) 2022-01-25
US20190002416A1 (en) 2019-01-03
MX2018010727A (es) 2019-01-24
US20220242836A1 (en) 2022-08-04
KR20220035991A (ko) 2022-03-22
RU2756223C2 (ru) 2021-09-28
DK3408260T3 (da) 2021-08-02
AU2017229466A1 (en) 2018-09-13
JP2019509286A (ja) 2019-04-04
CA3015505A1 (en) 2017-09-14
LT3408260T (lt) 2021-07-26
CO2018010568A2 (es) 2018-10-22
MY198185A (en) 2023-08-09
SMT202100434T1 (it) 2021-09-14
US20170275259A1 (en) 2017-09-28
HUE055546T2 (hu) 2021-12-28
KR20180114225A (ko) 2018-10-17
AU2017229466C1 (en) 2021-02-11
US10472335B2 (en) 2019-11-12
AU2017229466B2 (en) 2020-08-13
PL3408260T3 (pl) 2021-11-08
RU2018135072A (ru) 2020-04-08
CY1124397T1 (el) 2022-07-22
SI3408260T1 (sl) 2021-08-31
US12351561B2 (en) 2025-07-08
TW201741290A (zh) 2017-12-01
SG11201807591VA (en) 2018-10-30
RS62172B1 (sr) 2021-08-31

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