AU2018318990B2 - Corticotropin releasing factor receptor antagonists - Google Patents

Corticotropin releasing factor receptor antagonists Download PDF

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Publication number
AU2018318990B2
AU2018318990B2 AU2018318990A AU2018318990A AU2018318990B2 AU 2018318990 B2 AU2018318990 B2 AU 2018318990B2 AU 2018318990 A AU2018318990 A AU 2018318990A AU 2018318990 A AU2018318990 A AU 2018318990A AU 2018318990 B2 AU2018318990 B2 AU 2018318990B2
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AU
Australia
Prior art keywords
compound
pharmaceutical composition
pharmaceutically acceptable
solvate
acceptable salt
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.)
Ceased
Application number
AU2018318990A
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English (en)
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AU2018318990A1 (en
Inventor
Hal GERBER
Alexis HOWERTON
Sami Karaborni
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.)
Spruce Biosciences Inc
Original Assignee
Spruce Biosciences Inc
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Filing date
Publication date
Application filed by Spruce Biosciences Inc filed Critical Spruce Biosciences Inc
Publication of AU2018318990A1 publication Critical patent/AU2018318990A1/en
Application granted granted Critical
Publication of AU2018318990B2 publication Critical patent/AU2018318990B2/en
Priority to AU2023201703A priority Critical patent/AU2023201703B2/en
Priority to AU2024278470A priority patent/AU2024278470A1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2018318990A 2017-08-14 2018-08-14 Corticotropin releasing factor receptor antagonists Ceased AU2018318990B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2023201703A AU2023201703B2 (en) 2017-08-14 2023-03-20 Corticotropin releasing factor receptor antagonists
AU2024278470A AU2024278470A1 (en) 2017-08-14 2024-12-16 Corticotropin releasing factor receptor antagonists

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762545393P 2017-08-14 2017-08-14
US62/545,393 2017-08-14
PCT/US2018/046707 WO2019036472A1 (en) 2017-08-14 2018-08-14 CORTICOTROPIN RELEASE FACTOR RECEPTOR ANTAGONISTS

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2023201703A Division AU2023201703B2 (en) 2017-08-14 2023-03-20 Corticotropin releasing factor receptor antagonists

Publications (2)

Publication Number Publication Date
AU2018318990A1 AU2018318990A1 (en) 2019-11-21
AU2018318990B2 true AU2018318990B2 (en) 2023-01-05

Family

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Family Applications (3)

Application Number Title Priority Date Filing Date
AU2018318990A Ceased AU2018318990B2 (en) 2017-08-14 2018-08-14 Corticotropin releasing factor receptor antagonists
AU2023201703A Ceased AU2023201703B2 (en) 2017-08-14 2023-03-20 Corticotropin releasing factor receptor antagonists
AU2024278470A Abandoned AU2024278470A1 (en) 2017-08-14 2024-12-16 Corticotropin releasing factor receptor antagonists

Family Applications After (2)

Application Number Title Priority Date Filing Date
AU2023201703A Ceased AU2023201703B2 (en) 2017-08-14 2023-03-20 Corticotropin releasing factor receptor antagonists
AU2024278470A Abandoned AU2024278470A1 (en) 2017-08-14 2024-12-16 Corticotropin releasing factor receptor antagonists

Country Status (13)

Country Link
US (1) US20210137935A1 (enExample)
EP (1) EP3630763A4 (enExample)
JP (2) JP7285222B2 (enExample)
KR (1) KR102644781B1 (enExample)
CN (1) CN110997667A (enExample)
AR (1) AR112471A1 (enExample)
AU (3) AU2018318990B2 (enExample)
BR (1) BR112020002966A2 (enExample)
CA (1) CA3064445A1 (enExample)
EA (1) EA202090321A1 (enExample)
MX (2) MX2019015318A (enExample)
TW (2) TWI803504B (enExample)
WO (1) WO2019036472A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20210064407A (ko) 2014-01-21 2021-06-02 뉴로크린 바이오사이언시즈 인코퍼레이티드 선천성 부신 과형성 치료를 위한 ｃｒｆ1 수용체 길항제
BR112020002967A2 (pt) 2017-08-14 2020-08-11 Spruce Biosciences, Inc. antagonistas de receptor de fator de liberação de corticotropina
TWI803504B (zh) * 2017-08-14 2023-06-01 美商雲杉生物科技股份有限公司 促皮質素釋放因子受體拮抗劑
MX2020011344A (es) * 2018-04-27 2021-02-09 Spruce Biosciences Inc Métodos para tratar tumores en reposo suprarrenales testiculares y de ovarios.
PL3984523T3 (pl) 2018-12-07 2026-02-02 Neurocrine Biosciences, Inc. Antagonista receptora crf1, jego formulacje farmaceutyczne i postacie stałe do leczenia wrodzonego przerostu nadnerczy
KR20220052927A (ko) 2019-07-19 2022-04-28 스프루스 바이오사이언시스 인코포레이티드 선천성 부신 증식증의 치료 방법
US12383536B2 (en) 2019-09-27 2025-08-12 Neurocrine Biosciences, Inc. CRF receptor antagonists and methods of use
ES3039926T3 (en) 2019-12-04 2025-10-27 Neurocrine Biosciences Inc Crf receptor antagonists and methods of use
JP2023537598A (ja) 2020-08-12 2023-09-04 スプルース バイオサイエンシーズ，インク． 多嚢胞性卵巣症候群を処置するための方法および組成物
US20240024330A1 (en) * 2020-08-26 2024-01-25 Neurocrine Biosciences, Inc. Crf receptor antagonists and methods of use
US11708372B2 (en) 2021-11-19 2023-07-25 Spruce Biosciences, Inc. Crystalline composition of tildacerfont and methods of use and preparation thereof
WO2025188842A1 (en) * 2024-03-08 2025-09-12 Spruce Biosciences, Inc. Amorphous solid dispersion of tildacerfont formulations

Citations (1)

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Publication number Priority date Publication date Assignee Title
CN101516887A (zh) * 2006-09-20 2009-08-26 伊莱利利公司 作为crf1受体拮抗剂的噻唑吡唑并嘧啶类

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ES2168237T3 (es) 1996-02-07 2007-04-01 Neurocrine Biosciences, Inc. Pirazolopirimidinas como antagonistas de receptores de crf.
IL137019A0 (en) 1998-01-28 2001-06-14 Du Pont Pharm Co Azolo triazines and pyrimidines
IL137019A (en) * 1998-01-28 2010-11-30 Du Pont Pharm Co 2,7 - dimethyl - 4 - (substituted amino) - 8 - arylpyrazolo [1,5-a] triazine derivatives and pharmaceutical compositions containing them
HRP20010582A2 (en) * 1999-12-08 2002-08-31 Pharmacia Corp Valdecoxib compositions
JP2008503444A (ja) * 2004-02-13 2008-02-07 エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド Ｃｒｆ受容体アンタゴニスト、その調製法、その医薬組成物およびその使用
CN101142217B (zh) * 2005-03-21 2010-12-08 伊莱利利公司 咪唑并哒嗪化合物
MX2009003098A (es) * 2006-09-20 2009-04-01 Lilly Co Eli Compuestos de tiofen pirazolopirimidina.
TWI432435B (zh) * 2008-10-02 2014-04-01 Lilly Co Eli 作為合成中間物之噻唑基－吡唑并嘧啶化合物及相關合成方法
TWI803504B (zh) * 2017-08-14 2023-06-01 美商雲杉生物科技股份有限公司 促皮質素釋放因子受體拮抗劑

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Also Published As

Publication number Publication date
AU2024278470A1 (en) 2025-01-09
WO2019036472A1 (en) 2019-02-21
AU2023201703B2 (en) 2024-09-19
JP7285222B2 (ja) 2023-06-01
MX2019015318A (es) 2020-07-20
AR112471A1 (es) 2019-10-30
TW201925197A (zh) 2019-07-01
EP3630763A4 (en) 2021-03-10
MX2022015858A (es) 2023-01-24
KR102644781B1 (ko) 2024-03-06
CA3064445A1 (en) 2019-02-21
TWI803504B (zh) 2023-06-01
US20210137935A1 (en) 2021-05-13
JP2020530832A (ja) 2020-10-29
JP2023116489A (ja) 2023-08-22
EP3630763A1 (en) 2020-04-08
CN110997667A (zh) 2020-04-10
EA202090321A1 (ru) 2020-09-24
BR112020002966A2 (pt) 2020-08-11
JP7720354B2 (ja) 2025-08-07
KR20200038951A (ko) 2020-04-14
TW202400179A (zh) 2024-01-01
AU2018318990A1 (en) 2019-11-21
AU2023201703A1 (en) 2023-04-13

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired