WO2020111524A8 - 퓨로피리미딘 화합물의 염 및 결정형, 및 이의 약학적 용도 - Google Patents

퓨로피리미딘 화합물의 염 및 결정형, 및 이의 약학적 용도 Download PDF

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Publication number
WO2020111524A8
WO2020111524A8 PCT/KR2019/014164 KR2019014164W WO2020111524A8 WO 2020111524 A8 WO2020111524 A8 WO 2020111524A8 KR 2019014164 W KR2019014164 W KR 2019014164W WO 2020111524 A8 WO2020111524 A8 WO 2020111524A8
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WIPO (PCT)
Prior art keywords
salt
crystalline form
pharmaceutical use
compound
trifluoromethyl
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PCT/KR2019/014164
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English (en)
French (fr)
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WO2020111524A1 (ko
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이민희
김선미
김훈택
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주식회사 티움바이오
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Application filed by 주식회사 티움바이오 filed Critical 주식회사 티움바이오
Priority to JP2021530802A priority Critical patent/JP2022510928A/ja
Priority to ES19889945T priority patent/ES2952033T3/es
Priority to US17/296,836 priority patent/US20220002312A1/en
Priority to EP19889945.2A priority patent/EP3889157B1/en
Priority to CN201980078178.9A priority patent/CN113166172A/zh
Priority to CA3124684A priority patent/CA3124684A1/en
Publication of WO2020111524A1 publication Critical patent/WO2020111524A1/ko
Publication of WO2020111524A8 publication Critical patent/WO2020111524A8/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20—Spiro-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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/06—Oxalic acid
    • C07C55/07—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

본 발명에 따른 화학식 1의 화합물, 즉 (R)-4-((2-(1-(2-플루오로-6-(트리플루오로메틸)벤질)-2,4-디옥소-1'-((5-(트리플루오로메틸)퓨란-2-일)메틸)-1H-스피로[퓨로[3,4-d]피리미딘-5,4'-피페리딘]-3(2H,4H,7H)-일)-1-페닐에틸)아미노)부타논산의 염 및 결정형은 물리화학적 제반 특성, 즉 흡습도, 유연물질, 화학적 안정성 등의 면에서 우수하여, 이를 유효 성분으로 포함하는 약학적 조성물의 제조와 같은 약학적 용도에 이용될 수 있다.
PCT/KR2019/014164 2018-11-30 2019-10-25 퓨로피리미딘 화합물의 염 및 결정형, 및 이의 약학적 용도 WO2020111524A1 (ko)

Priority Applications (6)

Application Number Priority Date Filing Date Title
JP2021530802A JP2022510928A (ja) 2018-11-30 2019-10-25 フロピリミジン化合物の塩および結晶形ならびにその医薬用途
ES19889945T ES2952033T3 (es) 2018-11-30 2019-10-25 Sal y forma cristalina de un compuesto de furopirimidina y uso farmacéutico de estas
US17/296,836 US20220002312A1 (en) 2018-11-30 2019-10-25 Salt and crystalline form of furopyrimidine compound and pharmaceutical use thereof
EP19889945.2A EP3889157B1 (en) 2018-11-30 2019-10-25 Salt and crystalline form of furopyrimidine compound and pharmaceutical use thereof
CN201980078178.9A CN113166172A (zh) 2018-11-30 2019-10-25 嘌呤并嘧啶化合物的盐和晶型及其药物用途
CA3124684A CA3124684A1 (en) 2018-11-30 2019-10-25 Salt and crystalline form of furopyrimidine compound and pharmaceutical use thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020180151990A KR101973074B1 (ko) 2018-11-30 2018-11-30 퓨로피리미딘 화합물의 염 및 결정형, 및 이를 포함하는 약학적 조성물
KR10-2018-0151990 2018-11-30

Publications (2)

Publication Number Publication Date
WO2020111524A1 WO2020111524A1 (ko) 2020-06-04
WO2020111524A8 true WO2020111524A8 (ko) 2021-07-22

Family

ID=66281116

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2019/014164 WO2020111524A1 (ko) 2018-11-30 2019-10-25 퓨로피리미딘 화합물의 염 및 결정형, 및 이의 약학적 용도

Country Status (8)

Country Link
US (1) US20220002312A1 (ko)
EP (1) EP3889157B1 (ko)
JP (1) JP2022510928A (ko)
KR (1) KR101973074B1 (ko)
CN (1) CN113166172A (ko)
CA (1) CA3124684A1 (ko)
ES (1) ES2952033T3 (ko)
WO (1) WO2020111524A1 (ko)

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI225863B (en) * 1999-03-24 2005-01-01 Takeda Chemical Industries Ltd Thienopyrimidine compounds, their production and use
WO2001029044A1 (en) * 1999-10-15 2001-04-26 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
US9034850B2 (en) * 2009-11-20 2015-05-19 Sk Chemicals Co., Ltd. Gonadotropin releasing hormone receptor antagonist, preparation method thereof and pharmaceutical composition comprising the same
BR112014021331B1 (pt) * 2012-02-28 2020-12-15 Tiumbio Co., Ltd Antagonistas do receptor do hormônio liberador de gonadotropina, composição farmacêutica compreendendo os mesmos e uso desses
FR3037959B1 (fr) * 2015-06-23 2017-08-04 Servier Lab Nouveaux derives bicycliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent

Also Published As

Publication number Publication date
EP3889157A4 (en) 2022-08-31
CN113166172A (zh) 2021-07-23
EP3889157B1 (en) 2023-07-26
EP3889157A1 (en) 2021-10-06
KR101973074B1 (ko) 2019-04-26
CA3124684A1 (en) 2020-06-04
US20220002312A1 (en) 2022-01-06
JP2022510928A (ja) 2022-01-28
WO2020111524A1 (ko) 2020-06-04
EP3889157C0 (en) 2023-07-26
ES2952033T3 (es) 2023-10-26

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