CN115175912B - 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′-甲氧基脲的结晶溶剂化形式 - Google Patents

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′-甲氧基脲的结晶溶剂化形式 Download PDF

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CN115175912B
CN115175912B CN202080082800.6A CN202080082800A CN115175912B CN 115175912 B CN115175912 B CN 115175912B CN 202080082800 A CN202080082800 A CN 202080082800A CN 115175912 B CN115175912 B CN 115175912B
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crystalline form
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xiii
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CN115175912A (zh
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C·雅古施
C·K·赫兹
A·施罗德
P·I·弗拉霍瓦
S·斯蒂威斯
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Sumitomo Pharma Co Ltd
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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)
  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN202080082800.6A 2019-10-10 2020-10-09 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′-甲氧基脲的结晶溶剂化形式 Active CN115175912B (zh)

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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

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CN115175912B true CN115175912B (zh) 2025-04-11

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US (1) US20220372044A1 (https=)
EP (1) EP4041738A1 (https=)
JP (1) JP7713934B2 (https=)
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WO (1) WO2021069700A1 (https=)

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ES2912929T5 (en) 2016-09-30 2025-05-09 Sumitomo Pharma Switzerland Gmbh Methods of treating uterine fibroids and endometriosis
US12441738B2 (en) 2018-03-14 2025-10-14 Assia Chemical Industries Ltd. Solid state forms of Relugolix
JP2022551316A (ja) 2019-10-10 2022-12-08 ミオバント サイエンシズ ゲーエムベーハー 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形
CA3185151A1 (en) 2020-05-29 2021-12-02 Myovant Sciences Gmbh Combination solid oral dosage forms of gonadotropin-releasing hormone antagonists
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
JP2024540922A (ja) 2021-10-18 2024-11-06 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 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’－メトキシ尿素のエタノール溶媒和物の結晶形

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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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US7300935B2 (en) * 2003-01-29 2007-11-27 Takeda Pharmaceutical Company Thienopyrimidine compounds and use thereof
TWI508962B (zh) * 2009-04-22 2015-11-21 Du Pont 氮雜環醯胺之固體形態
NZ609490A (en) * 2010-10-21 2015-06-26 Biomarin Pharm Inc Crystalline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phthalazin-3(7h)-one tosylate salt
US20150099753A1 (en) * 2012-05-11 2015-04-09 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
AR092707A1 (es) * 2012-09-28 2015-04-29 Takeda Pharmaceuticals Co Metodo de produccion de derivado de tienopirimidina
ES2912929T5 (en) * 2016-09-30 2025-05-09 Sumitomo Pharma Switzerland Gmbh Methods of treating uterine fibroids and endometriosis
MA46361A (fr) * 2016-09-30 2021-03-31 Myovant Sciences Gmbh Traitement du cancer de la prostate
US11306104B2 (en) * 2018-03-14 2022-04-19 Teva Pharmaceuticals International Gmbh Solid state forms of Relugolix
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

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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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CN115175912A (zh) 2022-10-11
WO2021069700A1 (en) 2021-04-15
JP7713934B2 (ja) 2025-07-28
US20220372044A1 (en) 2022-11-24
JP2022551525A (ja) 2022-12-09
EP4041738A1 (en) 2022-08-17

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