KR101074462B1 - 티에노피리미딘 화합물 및 그 용도 - Google Patents

티에노피리미딘 화합물 및 그 용도 Download PDF

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KR101074462B1
KR101074462B1 KR1020057014100A KR20057014100A KR101074462B1 KR 101074462 B1 KR101074462 B1 KR 101074462B1 KR 1020057014100 A KR1020057014100 A KR 1020057014100A KR 20057014100 A KR20057014100 A KR 20057014100A KR 101074462 B1 KR101074462 B1 KR 101074462B1
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methyl
compound
mmol
phenyl
amino
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KR20050096171A (ko
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노부오 죠
다카시 이마다
다케노리 히타카
가즈히로 미와
마사미 구사카
노부히로 스즈키
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다케다 야쿠힌 고교 가부시키가이샤
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    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P15/16—Masculine 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
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A61P5/04—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
    • 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
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020057014100A 2003-01-29 2004-01-28 티에노피리미딘 화합물 및 그 용도 Expired - Lifetime KR101074462B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2003020854 2003-01-29
JPJP-P-2003-00020854 2003-01-29

Publications (2)

Publication Number Publication Date
KR20050096171A KR20050096171A (ko) 2005-10-05
KR101074462B1 true KR101074462B1 (ko) 2011-10-18

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KR1020057014100A Expired - Lifetime KR101074462B1 (ko) 2003-01-29 2004-01-28 티에노피리미딘 화합물 및 그 용도

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US (4) US7300935B2 (enExample)
EP (1) EP1591446B1 (enExample)
KR (1) KR101074462B1 (enExample)
CN (2) CN100360538C (enExample)
AU (1) AU2004207706B2 (enExample)
BE (1) BE2022C501I2 (enExample)
BR (1) BRPI0407082C1 (enExample)
CA (1) CA2514407C (enExample)
CO (1) CO5590921A2 (enExample)
CY (2) CY1114008T1 (enExample)
DK (1) DK1591446T3 (enExample)
ES (1) ES2410814T3 (enExample)
FR (1) FR21C1056I2 (enExample)
HU (1) HUS2100052I1 (enExample)
IL (1) IL169869A (enExample)
LT (1) LTC1591446I2 (enExample)
MX (1) MXPA05007990A (enExample)
NL (1) NL301158I2 (enExample)
NO (2) NO331981B1 (enExample)
NZ (1) NZ541772A (enExample)
PL (1) PL214756B1 (enExample)
PT (1) PT1591446E (enExample)
RU (1) RU2331648C2 (enExample)
SI (1) SI1591446T1 (enExample)
WO (1) WO2004067535A1 (enExample)
ZA (1) ZA200506611B (enExample)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6828415B2 (en) * 1993-02-19 2004-12-07 Zentaris Gmbh Oligopeptide lyophilisate, their preparation and use
US20090048273A1 (en) * 2005-07-22 2009-02-19 Takeda Pharmaceutical Company Limited Premature ovulation preventive agent
US20100061976A1 (en) * 2008-07-24 2010-03-11 Searete Llc, A Limited Liability Corporation Of The State Of Delaware Method for treating or preventing osteoporosis by reducing follicle stimulating hormone to cyclic physiological levels in a mammalian subject
WO2010026993A1 (ja) 2008-09-03 2010-03-11 武田薬品工業株式会社 製剤における吸収性改善方法および吸収性が改善された製剤
ME02230B (me) 2009-01-08 2016-02-20 Curis Inc Inhibitori fosfoinozitid 3-kinaze sa delom koji vezuje cink
WO2011153049A1 (en) 2010-06-02 2011-12-08 The Trustees Of The University Of Pennsylvania Methods and use of compounds that bind to her2/neu receptor complex
US9265739B2 (en) 2010-06-02 2016-02-23 The Trustees Of The University Of Pennsylvania Methods and use of compounds that bind to HER2/neu receptor complex
PE20141382A1 (es) 2011-04-01 2014-11-04 Curis Inc Inhibidor de la fosfoinositida-3-quinasa con un grupo de union a zinc
DK2776038T3 (en) * 2011-11-11 2018-04-23 Gilead Apollo Llc ACC INHIBITORS AND APPLICATIONS THEREOF
HUE044048T2 (hu) * 2012-09-28 2019-09-30 Takeda Pharmaceuticals Co Eljárás tienopirimidin származék elõállítására
US9468681B2 (en) 2013-03-01 2016-10-18 California Institute Of Technology Targeted nanoparticles
EP2881391A1 (en) 2013-12-05 2015-06-10 Bayer Pharma Aktiengesellschaft Spiroindoline carbocycle derivatives and pharmaceutical compositions thereof
EP4454708A3 (en) 2015-02-26 2024-11-13 Takeda Pharmaceutical Company Limited A tablet comprising a methoxyurea derivative and mannitol particles
ES2882255T3 (es) 2015-07-01 2021-12-01 California Inst Of Techn Sistemas de administración basados en polímeros de ácido múcico catiónicos
AR106472A1 (es) 2015-10-26 2018-01-17 Gilead Apollo Llc Inhibidores de acc y usos de los mismos
PT3380479T (pt) 2015-11-25 2023-03-13 Gilead Apollo Llc Inhibidores de triazol acc e seus usos
US20170166583A1 (en) 2015-11-25 2017-06-15 Gilead Apollo, Llc Ester acc inhibitors and uses thereof
US20170166582A1 (en) 2015-11-25 2017-06-15 Gilead Apollo, Llc Pyrazole acc inhibitors and uses thereof
US20170166585A1 (en) 2015-11-25 2017-06-15 Gilead Apollo, Llc Pesticidal compositions and uses thereof
RU2610281C1 (ru) * 2016-02-26 2017-02-08 ФЕДЕРАЛЬНОЕ ГОСУДАРСТВЕННОЕ БЮДЖЕТНОЕ УЧРЕЖДЕНИЕ НАУКИ ИНСТИТУТ ОРГАНИЧЕСКОЙ ХИМИИ им. Н.Д. ЗЕЛИНСКОГО РОССИЙСКОЙ АКАДЕМИИ НАУК (ИОХ РАН) Способ получения 2-фтор-3-метилбут-2-ениламина или его гидрохлорида (Варианты)
CN112920200A (zh) 2016-03-02 2021-06-08 吉利德阿波罗公司 噻吩并嘧啶二酮acc抑制剂的固体形式及其制备方法
HUE070578T2 (hu) 2016-09-30 2025-06-28 Sumitomo Pharma Switzerland Gmbh Prosztatarák kezelése
WO2018060501A2 (en) * 2016-09-30 2018-04-05 Myovant Sciences Gmbh Methods of treating uterine fibroids and endometriosis
JP6906626B2 (ja) 2017-03-28 2021-07-21 ギリアード サイエンシーズ， インコーポレイテッド 肝疾患を処置するための治療的組み合わせ
EA201992612A1 (ru) 2017-06-05 2020-05-20 Обсева С.А. Схемы применения антагониста гонадотропин-высвобождающего гормона для лечения эндометриоза
US12441738B2 (en) 2018-03-14 2025-10-14 Assia Chemical Industries Ltd. Solid state forms of Relugolix
US11306104B2 (en) 2018-03-14 2022-04-19 Teva Pharmaceuticals International Gmbh Solid state forms of Relugolix
US20190381188A1 (en) 2018-06-13 2019-12-19 California Institute Of Technology Nanoparticles For Crossing The Blood Brain Barrier And Methods Of Treatment Using The Same
CA3112177A1 (en) 2018-09-11 2020-03-19 Curis, Inc. Combination therapy with a phosphoinositide 3-kinase inhibitor with a zinc binding moiety
AU2019373349B2 (en) 2018-10-29 2025-01-09 Kissei Pharmaceutical Co., Ltd. Compositions and methods for the treatment of adenomyosis and rectovaginal endometriosis
US20230067378A1 (en) 2018-11-07 2023-03-02 ObsEva S.A. Compositions and methods for the treatment of estrogen-dependent disorders
EP3666776A1 (en) 2018-12-11 2020-06-17 Sandoz AG Hydrate of a gonadotropin-releasing hormone receptor antagonist
WO2020230094A1 (en) * 2019-05-15 2020-11-19 Dr. Reddy’S Laboratories Limited Amorphous and crystalline forms of relugolix
CN110194776B (zh) * 2019-06-27 2021-05-28 四川伊诺达博医药科技有限公司 一种瑞卢戈利的合成方法
CN111943960B (zh) * 2019-07-29 2022-02-15 广东东阳光药业有限公司 取代的嘧啶二酮类化合物及其用途
CA3145993A1 (en) * 2019-08-02 2021-02-11 Johnson Matthey Public Limited Company Solid-state forms of relugolix
CN112321602A (zh) * 2019-08-05 2021-02-05 苏州鹏旭医药科技有限公司 一种瑞卢戈利药物中间体的制备方法
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JP7713934B2 (ja) * 2019-10-10 2025-07-28 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’－メトキシ尿素の結晶溶媒和形
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
CN112745304A (zh) * 2019-10-29 2021-05-04 上海度德医药科技有限公司 一种Relugolix的制备方法及中间体化合物
CN113444105A (zh) * 2020-03-27 2021-09-28 南京海润医药有限公司 一种Relugolix的制备方法
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
CN111574534B (zh) * 2020-05-25 2021-06-04 东莞市东阳光新药研发有限公司 苯基取代的噻吩并[2,3-d]嘧啶-2,4(1H,3H)-二酮类化合物及其用途
WO2021239917A1 (en) 2020-05-29 2021-12-02 Myovant Sciences Gmbh Combination solid oral dosage forms of gonadotropin-releasing hormone antagonists
CN111875614B (zh) * 2020-07-03 2022-04-29 东莞市东阳光新药研发有限公司 杂环基取代的噻吩并[2,3-d]嘧啶-2,4(1H,3H)-二酮类化合物及其用途
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EP4243829A1 (en) 2020-11-11 2023-09-20 Myovant Sciences GmbH Methods of administering relugolix
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CN117285506A (zh) * 2022-07-14 2023-12-26 江西同和药业股份有限公司 一种瑞卢戈利中间体及其制备方法
CN115417883B (zh) * 2022-09-16 2024-08-27 浙江科聚生物医药有限公司 一种瑞卢戈利的晶型及其制备方法
WO2024126674A1 (en) 2022-12-15 2024-06-20 Medichem, S.A. Process for the preparation of relugolix
WO2024222827A1 (zh) * 2023-04-27 2024-10-31 山东绿叶制药有限公司 一种噻吩并嘧啶类化合物的盐型、晶型及其制备方法和应用

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002043766A1 (en) * 2000-11-29 2002-06-06 Takeda Chemical Industries, Ltd. Medicinal compositions and process for producing the same

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6048863A (en) * 1994-04-19 2000-04-11 Takeda Chemical Industries, Ltd. Condensed-ring thiophene derivatives and thienopyrimidine derivatives, their production and use
UY23948A1 (es) 1995-02-08 2001-10-25 Takeda Chemical Industries Ltd Derivados de anillos condensados de tiofeno su producción y uso.
RU2233284C2 (ru) * 1999-03-24 2004-07-27 Такеда Кемикал Индастриз, Лтд. Тиенопиримидиновые производные, способ их получения, фармацевтическая композиция и способ антагонизации гонадотропин-рилизинг гормона
TWI225863B (en) 1999-03-24 2005-01-01 Takeda Chemical Industries Ltd Thienopyrimidine compounds, their production and use
JP2001316391A (ja) * 2000-02-29 2001-11-13 Takeda Chem Ind Ltd チエノピリミジン誘導体の製造法
CN1173977C (zh) * 2000-02-29 2004-11-03 武田药品工业株式会社 制备噻吩并嘧啶衍生物的方法
JP2001354588A (ja) * 2000-04-13 2001-12-25 Takeda Chem Ind Ltd アルツハイマー病予防・治療剤
EP1393747A1 (en) * 2000-04-13 2004-03-03 Takeda Chemical Industries, Ltd. Preventives/remedies for alzheimer's disease
AU2001264264A1 (en) * 2000-06-14 2001-12-24 Takeda Chemical Industries Ltd. Sustained release compositions
JP2002068982A (ja) * 2000-06-14 2002-03-08 Takeda Chem Ind Ltd 徐放性組成物
US20030176360A1 (en) 2000-07-05 2003-09-18 Yasutaka Igari Medicinal preparations for treating sex hormone-dependent diseases
JP2002080397A (ja) * 2000-07-05 2002-03-19 Takeda Chem Ind Ltd 性ホルモン依存性疾患の治療用医薬製剤
JP2002167327A (ja) * 2000-09-22 2002-06-11 Takeda Chem Ind Ltd 固形製剤
AU2001288102A1 (en) * 2000-09-22 2002-04-02 Takeda Chemical Industries Ltd. Solid preparations
AU2002221139A1 (en) 2000-12-15 2002-06-24 Takeda Chemical Industries Ltd. Medicinal compositions of nonpeptidyl gonadotropin-releasing hormone agonist or antagonist, process for producing the same and use thereof
CA2433778A1 (en) 2001-02-14 2002-08-22 William Glen Harter Thieno'2,3-d pyrimidindione derivatives as matrix metalloproteinase inhibitors
WO2003064429A1 (en) 2002-01-30 2003-08-07 Takeda Chemical Industries, Ltd. Thienopyrimidines, process for preparing the same and use thereof
JP5072166B2 (ja) * 2002-01-30 2012-11-14 武田薬品工業株式会社 チエノピリミジン化合物、その製造法および用途
US20050159361A1 (en) 2002-03-11 2005-07-21 Takahito Hara Remedies for sex hormone-dependent disease
JP2004002321A (ja) * 2002-03-11 2004-01-08 Takeda Chem Ind Ltd 性ホルモン依存性疾患治療剤
EP1495768A4 (en) 2002-04-12 2007-12-05 Takeda Pharmaceutical MEANS FOR THE PREVENTION / TREATMENT OF HITZEWALLUNGEN
JP2004002377A (ja) * 2002-04-12 2004-01-08 Takeda Chem Ind Ltd ホットフラッシュ予防・治療剤

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002043766A1 (en) * 2000-11-29 2002-06-06 Takeda Chemical Industries, Ltd. Medicinal compositions and process for producing the same

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