JP7713934B2 - Ｎ－（４－（１－（２，６－ジフルオロベンジル）－５－（（ジメチルアミノ）メチル）－３－（６－メトキシ－３－ピリダジニル）－２，４－ジオキソ－１，２，３，４－テトラヒドロチエノ［２，３－ｄ］ピリミジン－６－イル）フェニル）－Ｎ’－メトキシ尿素の結晶溶媒和形 - Google Patents

Ｎ－（４－（１－（２，６－ジフルオロベンジル）－５－（（ジメチルアミノ）メチル）－３－（６－メトキシ－３－ピリダジニル）－２，４－ジオキソ－１，２，３，４－テトラヒドロチエノ［２，３－ｄ］ピリミジン－６－イル）フェニル）－Ｎ’－メトキシ尿素の結晶溶媒和形

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JP7713934B2
JP7713934B2 JP2022521570A JP2022521570A JP7713934B2 JP 7713934 B2 JP7713934 B2 JP 7713934B2 JP 2022521570 A JP2022521570 A JP 2022521570A JP 2022521570 A JP2022521570 A JP 2022521570A JP 7713934 B2 JP7713934 B2 JP 7713934B2
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compound
methoxyurea
tetrahydrothieno
difluorobenzyl
dioxo
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JPWO2021069700A5 (OSRAM
JP2022551525A (ja
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ヤグシュ、カルステン
クラウス ハーツ、クリスティアーン
シュロット、アンドレアス
アイ． ヴラホヴァ、ペティンカ
スターンウェイス、スヴェン
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スミトモ ファーマ スウィッツァーランド ゲーエムベーハー
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2022521570A 2019-10-10 2020-10-09 Ｎ－（４－（１－（２，６－ジフルオロベンジル）－５－（（ジメチルアミノ）メチル）－３－（６－メトキシ－３－ピリダジニル）－２，４－ジオキソ－１，２，３，４－テトラヒドロチエノ［２，３－ｄ］ピリミジン－６－イル）フェニル）－Ｎ’－メトキシ尿素の結晶溶媒和形 Active JP7713934B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962913606P 2019-10-10 2019-10-10
US62/913,606 2019-10-10
PCT/EP2020/078475 WO2021069700A1 (en) 2019-10-10 2020-10-09 Crystalline solvated forms of n-(4-(1-(2,6-difluorobenzyl)-5- ((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4- tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea

Publications (3)

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JP2022551525A JP2022551525A (ja) 2022-12-09
JPWO2021069700A5 JPWO2021069700A5 (OSRAM) 2023-10-17
JP7713934B2 true JP7713934B2 (ja) 2025-07-28

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JP2022521570A Active JP7713934B2 (ja) 2019-10-10 2020-10-09 Ｎ－（４－（１－（２，６－ジフルオロベンジル）－５－（（ジメチルアミノ）メチル）－３－（６－メトキシ－３－ピリダジニル）－２，４－ジオキソ－１，２，３，４－テトラヒドロチエノ［２，３－ｄ］ピリミジン－６－イル）フェニル）－Ｎ’－メトキシ尿素の結晶溶媒和形

Country Status (5)

Country Link
US (1) US20220372044A1 (OSRAM)
EP (1) EP4041738A1 (OSRAM)
JP (1) JP7713934B2 (OSRAM)
CN (1) CN115175912B (OSRAM)
WO (1) WO2021069700A1 (OSRAM)

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JP7043503B2 (ja) 2016-09-30 2022-03-29 ミオバント サイエンシズ ゲーエムベーハー 子宮筋腫及び子宮内膜症を治療する方法
US12441738B2 (en) 2018-03-14 2025-10-14 Assia Chemical Industries Ltd. Solid state forms of Relugolix
CN115279769A (zh) 2019-10-10 2022-11-01 梦欧文科学有限责任公司 N-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基-3-哒嗪基)-2,4-二氧代-1,2,3,4-四氢噻吩并[2,3-d]嘧啶-6-基)苯基)-n’-甲氧基脲的结晶形式
WO2022101303A1 (en) 2020-11-11 2022-05-19 Myovant Sciences Gmbh Methods of administering relugolix
CN113620972A (zh) * 2021-02-02 2021-11-09 奥锐特药业(天津)有限公司 瑞卢戈利新晶型及其制备方法
WO2022214645A1 (en) 2021-04-09 2022-10-13 Farmhispania Group, S.L. Processes and intermediates for the preparation of relugolix
WO2023066941A1 (en) 2021-10-18 2023-04-27 Myovant Sciences Gmbh Crystalline form of an ethanol solvate of n-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea

Citations (3)

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JP2015532262A (ja) 2012-09-28 2015-11-09 武田薬品工業株式会社 チエノピリミジン誘導体の製造方法
WO2018060463A2 (en) 2016-09-30 2018-04-05 Myovant Sciences Gmbh Treatment of prostate cancer
WO2019178304A1 (en) 2018-03-14 2019-09-19 Teva Pharmaceuticals International Gmbh Solid state forms of relugolix

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KR101074462B1 (ko) * 2003-01-29 2011-10-18 다케다 야쿠힌 고교 가부시키가이샤 티에노피리미딘 화합물 및 그 용도
TWI508962B (zh) * 2009-04-22 2015-11-21 Du Pont 氮雜環醯胺之固體形態
PT2630146T (pt) * 2010-10-21 2020-07-20 Medivation Tech Llc Sal tosilato de (8s,9r)-5-fluoro-8-(4-fluorofenil)-9-(1-metil-1h-1,2,4-triazol-5-il)-8,9-di-hidro-2h-pirido[4,3,2-de]ftalazin-3(7h)-ona cristalino
WO2013170243A1 (en) * 2012-05-11 2013-11-14 Concert Pharmaceuticals, Inc. Form 5 polymorph of 7-(tert-butyl-d9)-3-(2,5-difluorophenyl)-6((1-methyl-1h-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine
JP7043503B2 (ja) * 2016-09-30 2022-03-29 ミオバント サイエンシズ ゲーエムベーハー 子宮筋腫及び子宮内膜症を治療する方法
EP3666776A1 (en) * 2018-12-11 2020-06-17 Sandoz AG Hydrate of a gonadotropin-releasing hormone receptor antagonist
US20220220123A1 (en) * 2019-05-15 2022-07-14 Dr. Reddy's Laboratories Limited Amorphous and crystalline forms of relugolix
CN111423452B (zh) * 2020-03-26 2023-08-22 江西青峰药业有限公司 瑞卢戈利的中间体及其制备方法和应用
CN111333633B (zh) * 2020-04-01 2023-10-20 江西科睿药业有限公司 一种瑞卢戈利的中间体化合物及其制备方法和用途
CN115947734A (zh) * 2021-10-09 2023-04-11 江苏希迪制药有限公司 瑞卢戈利溶剂化物的晶型及其制备方法

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JP2015532262A (ja) 2012-09-28 2015-11-09 武田薬品工業株式会社 チエノピリミジン誘導体の製造方法
WO2018060463A2 (en) 2016-09-30 2018-04-05 Myovant Sciences Gmbh Treatment of prostate cancer
WO2019178304A1 (en) 2018-03-14 2019-09-19 Teva Pharmaceuticals International Gmbh Solid state forms of relugolix

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芦澤 一英，塩・結晶形の最適化と結晶化技術，Pharm Tech Japan，2002年，Vol. 18, No. 10，p. 81-96

Also Published As

Publication number Publication date
EP4041738A1 (en) 2022-08-17
WO2021069700A1 (en) 2021-04-15
CN115175912B (zh) 2025-04-11
CN115175912A (zh) 2022-10-11
US20220372044A1 (en) 2022-11-24
JP2022551525A (ja) 2022-12-09

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