TWI803504B - 促皮質素釋放因子受體拮抗劑 - Google Patents

促皮質素釋放因子受體拮抗劑 Download PDF

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Publication number
TWI803504B
TWI803504B TW107128345A TW107128345A TWI803504B TW I803504 B TWI803504 B TW I803504B TW 107128345 A TW107128345 A TW 107128345A TW 107128345 A TW107128345 A TW 107128345A TW I803504 B TWI803504 B TW I803504B
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Taiwan
Prior art keywords
compound
pharmaceutical formulation
pharmaceutically acceptable
solvate
acceptable salt
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TW107128345A
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English (en)
Chinese (zh)
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TW201925197A (zh
Inventor
艾莉西斯 霍爾頓
哈爾 嘉寶
薩米 卡拉波尼
Original Assignee
美商雲杉生物科技股份有限公司
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    • 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
    • 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; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (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)
TW107128345A 2017-08-14 2018-08-14 促皮質素釋放因子受體拮抗劑 TWI803504B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762545393P 2017-08-14 2017-08-14
US62/545,393 2017-08-14

Publications (2)

Publication Number Publication Date
TW201925197A TW201925197A (zh) 2019-07-01
TWI803504B true TWI803504B (zh) 2023-06-01

Family

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Family Applications (2)

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TW107128345A TWI803504B (zh) 2017-08-14 2018-08-14 促皮質素釋放因子受體拮抗劑
TW112117030A TW202400179A (zh) 2017-08-14 2018-08-14 促皮質素釋放因子受體拮抗劑

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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 (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3096756T (pt) 2014-01-21 2024-08-26 Neurocrine Biosciences Inc Antagonistas do recetor crf1 para o tratamento da hiperplasia adrenal congénita
BR112020002967A2 (pt) 2017-08-14 2020-08-11 Spruce Biosciences, Inc. antagonistas de receptor de fator de liberação de corticotropina
AU2018318990B2 (en) * 2017-08-14 2023-01-05 Spruce Biosciences, Inc. Corticotropin releasing factor receptor antagonists
WO2019210266A1 (en) * 2018-04-27 2019-10-31 Spruce Biosciences, Inc. Methods for treating testicular and ovarian adrenal rest tumors
MA54395A (fr) 2018-12-07 2022-03-16 Neurocrine Biosciences Inc Antagoniste du récepteur crf1, formulations pharmaceutiques et formes solides correspondantes pour le traitement de l'hyperplasie surrénalienne congénitale
EP3986416A4 (en) * 2019-07-19 2023-06-28 Spruce Biosciences, Inc. Methods of treating congenital adrenal hyperplasia
US12383536B2 (en) 2019-09-27 2025-08-12 Neurocrine Biosciences, Inc. CRF receptor antagonists and methods of use
WO2022036123A1 (en) 2020-08-12 2022-02-17 Spruce Biosciences, Inc. Methods and compositions for treating polycystic ovary syndrome
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030008885A1 (en) * 1996-07-24 2003-01-09 Liqi He Azolo triazines and pyrimidines
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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL123835A0 (en) 1996-02-07 1998-10-30 Janssen Pharmaceutica Nv Pyrazolopyrimidines as CRF receptor antagonists
CN1137123C (zh) 1998-01-28 2004-02-04 杜邦药品公司 吡咯并三嗪和嘧啶化合物
KR100664479B1 (ko) * 1999-12-08 2007-01-04 파마시아 코포레이션 발데콕시브 조성물
EP1722826A2 (en) * 2004-02-13 2006-11-22 SB Pharmco Puerto Rico Inc. Crf receptor antagonists, their preparations, their pharmaceutical composition and their uses
US7612067B2 (en) 2005-03-21 2009-11-03 Eli Lilly And Company Imidazopyridazine compounds
BRPI0717070A2 (pt) * 2006-09-20 2013-09-24 Lilly Co Eli compostos de tiofeno pirazolopirimidina
CA2739422C (en) * 2008-10-02 2013-03-12 Eli Lilly And Company Thiazolyl-pyrazolopyrimidine compounds as synthetic intermediates and related synthetic processes
AU2018318990B2 (en) * 2017-08-14 2023-01-05 Spruce Biosciences, Inc. Corticotropin releasing factor receptor antagonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030008885A1 (en) * 1996-07-24 2003-01-09 Liqi He Azolo triazines and pyrimidines
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

Also Published As

Publication number Publication date
CA3064445A1 (en) 2019-02-21
AU2024278470A1 (en) 2025-01-09
WO2019036472A1 (en) 2019-02-21
BR112020002966A2 (pt) 2020-08-11
MX2022015858A (es) 2023-01-24
AU2018318990B2 (en) 2023-01-05
JP7720354B2 (ja) 2025-08-07
CN110997667A (zh) 2020-04-10
AU2023201703B2 (en) 2024-09-19
EP3630763A4 (en) 2021-03-10
TW202400179A (zh) 2024-01-01
KR20200038951A (ko) 2020-04-14
KR102644781B1 (ko) 2024-03-06
AU2018318990A1 (en) 2019-11-21
EA202090321A1 (ru) 2020-09-24
US20210137935A1 (en) 2021-05-13
JP7285222B2 (ja) 2023-06-01
MX2019015318A (es) 2020-07-20
JP2023116489A (ja) 2023-08-22
AU2023201703A1 (en) 2023-04-13
AR112471A1 (es) 2019-10-30
TW201925197A (zh) 2019-07-01
JP2020530832A (ja) 2020-10-29
EP3630763A1 (en) 2020-04-08

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