JP2023549196A - レルゴリクスの投与方法 - Google Patents

レルゴリクスの投与方法 Download PDF

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Publication number
JP2023549196A
JP2023549196A JP2023528189A JP2023528189A JP2023549196A JP 2023549196 A JP2023549196 A JP 2023549196A JP 2023528189 A JP2023528189 A JP 2023528189A JP 2023528189 A JP2023528189 A JP 2023528189A JP 2023549196 A JP2023549196 A JP 2023549196A
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Prior art keywords
pharmaceutically acceptable
inhibitor
methoxy
dioxo
pyridazinyl
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JP2023528189A
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Japanese (ja)
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JP2023549196A5 (enExample
Inventor
エム． ミゴヤ、エリザベス
ビー． バックリー、デヴィッド
フェレイラ、フアン カミーロ アルホナ
イ、テン－イ
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ミオバント サイエンシズ ゲーエムベーハー
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Publication of JP2023549196A publication Critical patent/JP2023549196A/ja
Publication of JP2023549196A5 publication Critical patent/JP2023549196A5/ja
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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
    • A61K31/495—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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • 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
    • A61P5/30—Oestrogens
    • 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
    • A61P5/34—Gestagens

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2023528189A 2020-11-11 2021-11-10 レルゴリクスの投与方法 Pending JP2023549196A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202063112523P 2020-11-11 2020-11-11
US63/112,523 2020-11-11
US202163151423P 2021-02-19 2021-02-19
US63/151,423 2021-02-19
PCT/EP2021/081304 WO2022101303A1 (en) 2020-11-11 2021-11-10 Methods of administering relugolix

Publications (2)

Publication Number Publication Date
JP2023549196A true JP2023549196A (ja) 2023-11-22
JP2023549196A5 JP2023549196A5 (enExample) 2024-11-15

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JP2023528189A Pending JP2023549196A (ja) 2020-11-11 2021-11-10 レルゴリクスの投与方法

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EP (1) EP4243829A1 (enExample)
JP (1) JP2023549196A (enExample)
WO (1) WO2022101303A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018060501A2 (en) 2016-09-30 2018-04-05 Myovant Sciences Gmbh Methods of treating uterine fibroids and endometriosis
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
WO2021069700A1 (en) 2019-10-10 2021-04-15 Myovant Sciences Gmbh 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
BR112022023937A2 (pt) 2020-05-29 2022-12-27 Myovant Sciences Gmbh Formas de dosagem oral sólidas de combinação de antagonistas do hormônio liberador de gonadotropina

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019529574A (ja) * 2016-09-30 2019-10-17 ミオバント サイエンシズ ゲーエムベーハー 前立腺がんの治療
JP2020522571A (ja) * 2017-06-05 2020-07-30 オブセヴァ エス．エー． 子宮内膜症の治療のためのゴナドトロピン放出ホルモンアンタゴニスト投与計画

Family Cites Families (8)

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Publication number Priority date Publication date Assignee Title
CN101153042A (zh) 2003-01-29 2008-04-02 武田药品工业株式会社 噻吩并嘧啶化合物及其用途
SMT202200255T1 (it) 2012-09-28 2022-07-21 Takeda Pharmaceuticals Co Forma cristallina di 1-(4-1-(2,6-difluorobenzil)-5-dimetilamminometil-3-(6-metossipiridazin-3-il)-2,4-diosso-1,2,3,4-tetraidrotieno(2,3-d)-pirimidin-6il)fenil)-3-metossiurea
TWI744224B (zh) 2015-02-26 2021-11-01 日商武田藥品工業股份有限公司 固形製劑
WO2017040841A1 (en) * 2015-09-01 2017-03-09 Abbvie Inc. Methods of administering elagolix
WO2018060501A2 (en) 2016-09-30 2018-04-05 Myovant Sciences Gmbh Methods of treating uterine fibroids and endometriosis
TW201919632A (zh) * 2017-08-18 2019-06-01 美商艾伯維有限公司 治療子宮內膜異位症、子宮纖維瘤、多囊性卵巢症候群或子宮腺肌症之醫藥調配物
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
WO2021069700A1 (en) 2019-10-10 2021-04-15 Myovant Sciences Gmbh 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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019529574A (ja) * 2016-09-30 2019-10-17 ミオバント サイエンシズ ゲーエムベーハー 前立腺がんの治療
JP2020522571A (ja) * 2017-06-05 2020-07-30 オブセヴァ エス．エー． 子宮内膜症の治療のためのゴナドトロピン放出ホルモンアンタゴニスト投与計画

Non-Patent Citations (4)

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Title
"レルミナ錠４０ｍｇ", 添付文書, vol. 第5版, JPN6025051522, September 2020 (2020-09-01), pages 1 - 4, ISSN: 0005880627 *
LUKES, A. S. ET AL.: "Treatment of symptoms of uterine fibroids with relugolix combination therapy: efficacy and safety re", ASRM ABSTRACTS, vol. 112, no. 3, JPN6025051520, 2019, pages 434, ISSN: 0005753935 *
MACLEAN, D. B. ET AL.: " Medical castration using the investigational oral GnRH antagonist TAK-385 (Relugolix): phase 1 stud", J. CLIN. ENDOCRINOL METAB., vol. 100, no. 12, JPN6025051523, 2015, pages 4579 - 4587, ISSN: 0005753934 *
MIWA, K. ET AL.: "Discovery of 1-{4[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-d", J. MED. CHEM., vol. 54, JPN6025051521, 2011, pages 4998 - 5012, ISSN: 0005753936 *

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WO2022101303A1 (en) 2022-05-19

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