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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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)
  • 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)
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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Cited By (1)

* 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

Families Citing this family (10)

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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
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

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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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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
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
BRPI0717070A2 (pt) * 2006-09-20 2013-09-24 Lilly Co Eli compostos de tiofeno pirazolopirimidina
AU2018318990B2 (en) * 2017-08-14 2023-01-05 Spruce Biosciences, Inc. Corticotropin releasing factor receptor antagonists

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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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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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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
TWI803504B (zh) 2023-06-01
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
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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