JP7285222B2 - 副腎皮質刺激ホルモン放出因子受容体拮抗薬 - Google Patents

副腎皮質刺激ホルモン放出因子受容体拮抗薬 Download PDF

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JP7285222B2
JP7285222B2 JP2019572820A JP2019572820A JP7285222B2 JP 7285222 B2 JP7285222 B2 JP 7285222B2 JP 2019572820 A JP2019572820 A JP 2019572820A JP 2019572820 A JP2019572820 A JP 2019572820A JP 7285222 B2 JP7285222 B2 JP 7285222B2
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JP2020530832A (ja
JP2020530832A5 (enExample
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ハワートン，アレキシス
ゲルバー，ハル
カラボルニ，サミ
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スプルース バイオサイエンシズ インコーポレイテッド
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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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (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)
JP2019572820A 2017-08-14 2018-08-14 副腎皮質刺激ホルモン放出因子受容体拮抗薬 Active JP7285222B2 (ja)

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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

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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)
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Cited By (1)

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Publication number Priority date Publication date Assignee Title
JP2023116489A (ja) * 2017-08-14 2023-08-22 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

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CA3155599A1 (en) 2014-01-21 2015-07-30 Neurocrine Biosciences, Inc. Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia
BR112020002967A2 (pt) 2017-08-14 2020-08-11 Spruce Biosciences, Inc. antagonistas de receptor de fator de liberação de corticotropina
CN112423747A (zh) * 2018-04-27 2021-02-26 云杉生物科学公司 用于治疗睾丸肾上腺残余瘤和卵巢肾上腺残余瘤的方法
MA56226A (fr) 2018-12-07 2022-04-20 Neurocrine Biosciences Inc Antagoniste du récepteur crf1, formulations pharmaceutiques et ses formes solides pour le traitement de l'hyperplasie surrénale congénitale
KR20220052927A (ko) 2019-07-19 2022-04-28 스프루스 바이오사이언시스 인코포레이티드 선천성 부신 증식증의 치료 방법
CN118252829A (zh) 2019-09-27 2024-06-28 纽罗克里生物科学有限公司 Crf受体拮抗剂及使用方法
EP4656192A2 (en) * 2020-08-12 2025-12-03 Spruce Biosciences, Inc. Tildacerfont and derivatives thereof 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

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JP2000503661A (ja) 1996-02-07 2000-03-28 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｃｒｆレセプター拮抗薬としてのピラゾロピリミジン類
JP2002501922A (ja) 1998-01-28 2002-01-22 デュポン ファーマシューティカルズ カンパニー アゾロトリアジン類およびアゾロピリミジン類
JP2008533201A (ja) 2005-03-21 2008-08-21 イーライ リリー アンド カンパニー イミダゾピリダジン化合物
JP2010504344A (ja) 2006-09-20 2010-02-12 イーライ リリー アンド カンパニー Ｃｒｆ１受容体アンタゴニストとしてのチアゾールピラゾロピリミジン
JP2012504626A (ja) 2008-10-02 2012-02-23 イーライ リリー アンド カンパニー 合成中間体としてのチアゾリル−ピラゾロピリミジン化合物および関連合成方法

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JP2002501922A (ja) 1998-01-28 2002-01-22 デュポン ファーマシューティカルズ カンパニー アゾロトリアジン類およびアゾロピリミジン類
JP2008533201A (ja) 2005-03-21 2008-08-21 イーライ リリー アンド カンパニー イミダゾピリダジン化合物
JP2010504344A (ja) 2006-09-20 2010-02-12 イーライ リリー アンド カンパニー Ｃｒｆ１受容体アンタゴニストとしてのチアゾールピラゾロピリミジン
JP2012504626A (ja) 2008-10-02 2012-02-23 イーライ リリー アンド カンパニー 合成中間体としてのチアゾリル−ピラゾロピリミジン化合物および関連合成方法

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023116489A (ja) * 2017-08-14 2023-08-22 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
JP7720354B2 (ja) 2017-08-14 2025-08-07 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

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AU2024278470A1 (en) 2025-01-09
JP2023116489A (ja) 2023-08-22
MX2019015318A (es) 2020-07-20
EP3630763A4 (en) 2021-03-10
CN110997667A (zh) 2020-04-10
TWI803504B (zh) 2023-06-01
BR112020002966A2 (pt) 2020-08-11
AR112471A1 (es) 2019-10-30
JP2020530832A (ja) 2020-10-29
TW202400179A (zh) 2024-01-01
KR20200038951A (ko) 2020-04-14
AU2018318990A1 (en) 2019-11-21
EP3630763A1 (en) 2020-04-08
AU2018318990B2 (en) 2023-01-05
AU2023201703A1 (en) 2023-04-13
MX2022015858A (es) 2023-01-24
US20210137935A1 (en) 2021-05-13
CA3064445A1 (en) 2019-02-21
KR102644781B1 (ko) 2024-03-06
EA202090321A1 (ru) 2020-09-24
AU2023201703B2 (en) 2024-09-19
JP7720354B2 (ja) 2025-08-07
TW201925197A (zh) 2019-07-01
WO2019036472A1 (en) 2019-02-21

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