TW202400179A - 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
TW202400179A
TW202400179A TW112117030A TW112117030A TW202400179A TW 202400179 A TW202400179 A TW 202400179A TW 112117030 A TW112117030 A TW 112117030A TW 112117030 A TW112117030 A TW 112117030A TW 202400179 A TW202400179 A TW 202400179A
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TW
Taiwan
Prior art keywords
pharmaceutical composition
compound
pharmaceutically acceptable
solvate
acceptable salt
Prior art date
Application number
TW112117030A
Other languages
English (en)
Chinese (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
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 美商雲杉生物科技股份有限公司 filed Critical 美商雲杉生物科技股份有限公司
Publication of TW202400179A publication Critical patent/TW202400179A/zh

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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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Inorganic Chemistry (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)
TW112117030A 2017-08-14 2018-08-14 促皮質素釋放因子受體拮抗劑 TW202400179A (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 (1)

Publication Number Publication Date
TW202400179A true TW202400179A (zh) 2024-01-01

Family

ID=65362465

Family Applications (2)

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

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW107128345A TWI803504B (zh) 2017-08-14 2018-08-14 促皮質素釋放因子受體拮抗劑

Country Status (13)

Country Link
US (1) US20210137935A1 (https=)
EP (1) EP3630763A4 (https=)
JP (2) JP7285222B2 (https=)
KR (1) KR102644781B1 (https=)
CN (1) CN110997667A (https=)
AR (1) AR112471A1 (https=)
AU (3) AU2018318990B2 (https=)
BR (1) BR112020002966A2 (https=)
CA (1) CA3064445A1 (https=)
EA (1) EA202090321A1 (https=)
MX (2) MX2019015318A (https=)
TW (2) TW202400179A (https=)
WO (1) WO2019036472A1 (https=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS65839B1 (sr) 2014-01-21 2024-09-30 Neurocrine Biosciences Inc Crf1 receptor antagonisti za tretman kongenitalne adrenalne hiperplazije
JP7285222B2 (ja) * 2017-08-14 2023-06-01 スプルース バイオサイエンシズ インコーポレイテッド 副腎皮質刺激ホルモン放出因子受容体拮抗薬
WO2019036503A1 (en) 2017-08-14 2019-02-21 Spruce Biosciences, Inc. CORTICOTROPIN RELEASE FACTOR RECEPTOR ANTAGONISTS
EP4643950A3 (en) * 2018-04-27 2026-01-14 Spruce Biosciences, Inc. Methods for treating testicular and ovarian adrenal rest tumors
US20220023266A1 (en) 2018-12-07 2022-01-27 Neurocrine Biosciences, Inc. Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia
JP2022541550A (ja) * 2019-07-19 2022-09-26 スプルース バイオサイエンシーズ，インク． 先天性副腎過形成を処置する方法
JP7623365B2 (ja) 2019-09-27 2025-01-28 ニューロクライン バイオサイエンシーズ，インコーポレイテッド Ｃｒｆ受容体アンタゴニストおよび使用方法
KR20240023691A (ko) 2020-08-12 2024-02-22 스프루스 바이오사이언시스 인코포레이티드 다낭성 난소 증후군을 치료하기 위한 방법 및 조성물
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

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU713673B2 (en) 1996-02-07 1999-12-09 Neurocrine Biosciences Inc. Pyrazolopyrimidines as crf receptor antagonists
ATE301657T1 (de) 1998-01-28 2005-08-15 Bristol Myers Squibb Pharma Co Azolo-pyrimidine
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
PL351069A1 (en) * 1999-12-08 2003-03-10 Pharmacia Corp Valdecoxib compositions
EP1722826A2 (en) * 2004-02-13 2006-11-22 SB Pharmco Puerto Rico Inc. Crf receptor antagonists, their preparations, their pharmaceutical composition and their uses
EP1869049B1 (en) * 2005-03-21 2009-03-04 Eli Lilly And Company Imidazopyridazine compounds
HRP20100516T1 (hr) * 2006-09-20 2010-10-31 Eli Lilly And Company Tiazolpirazolopirimidini kao antagonisti receptora crf1
JP5184536B2 (ja) * 2006-09-20 2013-04-17 イーライ リリー アンド カンパニー チオフェンピラゾロピリミジン化合物
DK2350079T3 (da) * 2008-10-02 2012-12-17 Lilly Co Eli Thiazolylpyrazolopyrimidinforbindelser som syntetiske mellemprodukter og dertil relaterede syntetiske fremgangsmåder
JP7285222B2 (ja) 2017-08-14 2023-06-01 スプルース バイオサイエンシズ インコーポレイテッド 副腎皮質刺激ホルモン放出因子受容体拮抗薬

Also Published As

Publication number Publication date
AR112471A1 (es) 2019-10-30
JP7285222B2 (ja) 2023-06-01
JP2020530832A (ja) 2020-10-29
AU2024278470A1 (en) 2025-01-09
CN110997667A (zh) 2020-04-10
JP2023116489A (ja) 2023-08-22
AU2023201703B2 (en) 2024-09-19
KR102644781B1 (ko) 2024-03-06
EP3630763A1 (en) 2020-04-08
EA202090321A1 (ru) 2020-09-24
EP3630763A4 (en) 2021-03-10
TW201925197A (zh) 2019-07-01
AU2018318990B2 (en) 2023-01-05
MX2022015858A (es) 2023-01-24
WO2019036472A1 (en) 2019-02-21
KR20200038951A (ko) 2020-04-14
MX2019015318A (es) 2020-07-20
AU2018318990A1 (en) 2019-11-21
TWI803504B (zh) 2023-06-01
CA3064445A1 (en) 2019-02-21
US20210137935A1 (en) 2021-05-13
JP7720354B2 (ja) 2025-08-07
BR112020002966A2 (pt) 2020-08-11
AU2023201703A1 (en) 2023-04-13

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