KR102644781B1 - 코티코트로핀 방출 인자 수용체 길항제 - Google Patents

코티코트로핀 방출 인자 수용체 길항제 Download PDF

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KR102644781B1
KR102644781B1 KR1020207005534A KR20207005534A KR102644781B1 KR 102644781 B1 KR102644781 B1 KR 102644781B1 KR 1020207005534 A KR1020207005534 A KR 1020207005534A KR 20207005534 A KR20207005534 A KR 20207005534A KR 102644781 B1 KR102644781 B1 KR 102644781B1
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compound
delete delete
pharmaceutically acceptable
solvate
acceptable salt
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KR20200038951A (ko
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알렉시스 하워턴
할 거버
사미 카라보르니
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스프루스 바이오사이언시스 인코포레이티드
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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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physiology (AREA)
  • Nutrition Science (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)
KR1020207005534A 2017-08-14 2018-08-14 코티코트로핀 방출 인자 수용체 길항제 Active KR102644781B1 (ko)

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 (2)

Publication Number Publication Date
KR20200038951A KR20200038951A (ko) 2020-04-14
KR102644781B1 true KR102644781B1 (ko) 2024-03-06

Family

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KR1020207005534A Active KR102644781B1 (ko) 2017-08-14 2018-08-14 코티코트로핀 방출 인자 수용체 길항제

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) TW202400179A (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
CA3155599A1 (en) 2014-01-21 2015-07-30 Neurocrine Biosciences, Inc. Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia
KR102644781B1 (ko) * 2017-08-14 2024-03-06 스프루스 바이오사이언시스 인코포레이티드 코티코트로핀 방출 인자 수용체 길항제
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100022560A1 (en) 2006-09-20 2010-01-28 Zhaogen Chen Thiophene pyrazolopyrimidine compounds
US20110166345A1 (en) 2008-10-02 2011-07-07 Eli Lilly And Company Thiazolyl-pyrazolopyrimidine compounds as synthetic intermediates and related synthetic processes

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL191271B1 (pl) * 1996-02-07 2006-04-28 Neurocrine Biosciences Inc Pochodna pirazolopirymidyny i jej zastosowanie oraz kompozycja farmaceutyczna
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
ATE301657T1 (de) * 1998-01-28 2005-08-15 Bristol Myers Squibb Pharma Co Azolo-pyrimidine
CN1679556A (zh) * 1999-12-08 2005-10-12 法马西亚公司 维得克西组合物
WO2005079868A2 (en) * 2004-02-13 2005-09-01 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
JP5161226B2 (ja) * 2006-09-20 2013-03-13 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
KR102644781B1 (ko) 2017-08-14 2024-03-06 스프루스 바이오사이언시스 인코포레이티드 코티코트로핀 방출 인자 수용체 길항제

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100022560A1 (en) 2006-09-20 2010-01-28 Zhaogen Chen Thiophene pyrazolopyrimidine compounds
US20110166345A1 (en) 2008-10-02 2011-07-07 Eli Lilly And Company Thiazolyl-pyrazolopyrimidine compounds as synthetic intermediates and related synthetic processes

Also Published As

Publication number Publication date
AU2024278470A1 (en) 2025-01-09
JP2023116489A (ja) 2023-08-22
MX2019015318A (es) 2020-07-20
JP7285222B2 (ja) 2023-06-01
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
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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