CN110997667A - 促肾上腺皮质激素释放因子受体拮抗剂 - Google Patents

促肾上腺皮质激素释放因子受体拮抗剂 Download PDF

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Publication number
CN110997667A
CN110997667A CN201880038596.0A CN201880038596A CN110997667A CN 110997667 A CN110997667 A CN 110997667A CN 201880038596 A CN201880038596 A CN 201880038596A CN 110997667 A CN110997667 A CN 110997667A
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China
Prior art keywords
pharmaceutical composition
compound
pharmaceutically acceptable
solvate
acceptable salt
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Pending
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CN201880038596.0A
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English (en)
Chinese (zh)
Inventor
A·豪尔顿
H·格伯
S·卡拉博尼
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Spruce Biosciences Inc
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Spruce Biosciences Inc
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Publication of CN110997667A publication Critical patent/CN110997667A/zh
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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
    • A61K31/535—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
    • 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
    • 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

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  • 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)
CN201880038596.0A 2017-08-14 2018-08-14 促肾上腺皮质激素释放因子受体拮抗剂 Pending CN110997667A (zh)

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

Publications (1)

Publication Number Publication Date
CN110997667A true CN110997667A (zh) 2020-04-10

Family

ID=65362465

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880038596.0A Pending CN110997667A (zh) 2017-08-14 2018-08-14 促肾上腺皮质激素释放因子受体拮抗剂

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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101142217A (zh) * 2005-03-21 2008-03-12 伊莱利利公司 咪唑并哒嗪化合物
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
CN102171212A (zh) * 2008-10-02 2011-08-31 伊莱利利公司 作为合成中间体的噻唑基吡唑并嘧啶化合物及相关的合成方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
MX2009003098A (es) * 2006-09-20 2009-04-01 Lilly Co Eli Compuestos de tiofen pirazolopirimidina.
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101142217A (zh) * 2005-03-21 2008-03-12 伊莱利利公司 咪唑并哒嗪化合物
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
CN102171212A (zh) * 2008-10-02 2011-08-31 伊莱利利公司 作为合成中间体的噻唑基吡唑并嘧啶化合物及相关的合成方法

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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
EA202090321A1 (ru) 2020-09-24
BR112020002966A2 (pt) 2020-08-11
JP7720354B2 (ja) 2025-08-07
KR20200038951A (ko) 2020-04-14
AU2018318990B2 (en) 2023-01-05
TW202400179A (zh) 2024-01-01
AU2018318990A1 (en) 2019-11-21
AU2023201703A1 (en) 2023-04-13

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Application publication date: 20200410