NO20056251L - Pyrimidin-2,4-dionderivater som gonadotropin-frigjorende hormon reseptor antagonist - Google Patents

Pyrimidin-2,4-dionderivater som gonadotropin-frigjorende hormon reseptor antagonist

Info

Publication number
NO20056251L
NO20056251L NO20056251A NO20056251A NO20056251L NO 20056251 L NO20056251 L NO 20056251L NO 20056251 A NO20056251 A NO 20056251A NO 20056251 A NO20056251 A NO 20056251A NO 20056251 L NO20056251 L NO 20056251L
Authority
NO
Norway
Prior art keywords
gonadotropin
releasing hormone
pyrimidine
receptor antagonist
hormone receptor
Prior art date
Application number
NO20056251A
Other languages
English (en)
Other versions
NO334897B1 (no
Inventor
Chen Chen
Charles Q Huang
Zhiqiang Guo
Fabio C Tucci
Dongpei Wu
Yongsheng Chen
Warren Wade
Wesley J Dwight
Original Assignee
Neurocrine Biosciences Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34079121&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO20056251(L) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Neurocrine Biosciences Inc filed Critical Neurocrine Biosciences Inc
Publication of NO20056251L publication Critical patent/NO20056251L/no
Publication of NO334897B1 publication Critical patent/NO334897B1/no

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • 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
    • A61P15/08—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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

GnRH-reseptorantagonister er beskrevet og de kan anvendes for behandling av forskjellige tilstander vedrørende kjønnshormoner i både menn og kvinner. Forbindelsene ifølge denne oppfinnelsen har strukturen: hvor Ru, R-ib, R, R;,, Ra* Rj. RR, Rog X er som definert heri, inkludert stereoisomerer, prodroger og farmasøytisk akseptable salter derav. Også beskrevet er sammensetninger inneholdende en forbindelse ifølge denne oppfinnelsen i kombinasjon med en farmasøytisk akseptabel bærer, samt fremgangsmåter vedrørende anvendelse derav for antagonisering av gonadotropinfrigjørende hormon i et individ som trenger dette.
NO20056251A 2003-07-07 2005-12-30 Pyrimidin-2,4-dionderivater samt anvendelse derav og farmasøytisk sammensetning NO334897B1 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US48543403P 2003-07-07 2003-07-07
PCT/US2004/021593 WO2005007165A1 (en) 2003-07-07 2004-07-06 Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists

Publications (2)

Publication Number Publication Date
NO20056251L true NO20056251L (no) 2006-01-31
NO334897B1 NO334897B1 (no) 2014-06-30

Family

ID=34079121

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20056251A NO334897B1 (no) 2003-07-07 2005-12-30 Pyrimidin-2,4-dionderivater samt anvendelse derav og farmasøytisk sammensetning

Country Status (24)

Country Link
US (3) US7056927B2 (no)
EP (1) EP1646389B1 (no)
JP (2) JP4722844B2 (no)
KR (1) KR101139148B1 (no)
CN (1) CN100424078C (no)
AT (1) ATE407679T1 (no)
AU (1) AU2004257639B2 (no)
BR (1) BRPI0412314B8 (no)
CA (1) CA2531508C (no)
CY (1) CY1108656T1 (no)
DE (1) DE602004016516D1 (no)
DK (1) DK1646389T3 (no)
EA (1) EA010370B1 (no)
ES (1) ES2314448T3 (no)
HR (1) HRP20080646T3 (no)
IL (1) IL172833A (no)
MX (1) MXPA06000297A (no)
NO (1) NO334897B1 (no)
NZ (1) NZ544747A (no)
PL (1) PL1646389T3 (no)
PT (1) PT1646389E (no)
SI (1) SI1646389T1 (no)
WO (1) WO2005007165A1 (no)
ZA (1) ZA200600475B (no)

Families Citing this family (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4931314B2 (ja) * 2000-01-25 2012-05-16 ニューロクライン バイオサイエンシーズ，インコーポレイテッド 性腺刺激ホルモン放出ホルモンレセプタアンタゴニストおよびそれに関連した方法
CN100424078C (zh) * 2003-07-07 2008-10-08 纽罗克里生物科学有限公司 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物
WO2005007633A1 (en) * 2003-07-07 2005-01-27 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
CN100376246C (zh) 2003-07-07 2008-03-26 纽罗克里生物科学有限公司 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物
CN102127053A (zh) * 2004-03-15 2011-07-20 武田药品工业株式会社 二肽基肽酶抑制剂
WO2008124614A1 (en) 2007-04-06 2008-10-16 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
CL2008000985A1 (es) 2007-04-06 2008-10-10 Neurocrine Biosciences Inc Compuesto derivado de heterociclos de nitrogeno, agonistas del receptor gnrh; composicion farmaceutica que comprende a dicho compuesto; y uso para tratar una afeccion relacionada con las hormonas sexuales, endometriosis, dismenorrea, enfermedad de ov
CA2715080C (en) 2007-09-28 2021-09-28 Intrexon Corporation Therapeutic gene-switch constructs and bioreactors for the expression of biotherapeutic molecules, and uses thereof
US8765948B2 (en) * 2007-11-07 2014-07-01 Neurocrine Biosciences, Inc. Processes for the preparation of uracil derivatives
WO2011062437A2 (ko) * 2009-11-20 2011-05-26 에스케이케미칼주식회사 고나도트로핀 방출 호르몬 수용체 길항제, 이의 제조방법 및 이를 함유하는 약제학적 조성물
JP6159870B2 (ja) 2013-03-15 2017-07-05 アッヴィ・インコーポレイテッド 月経出血過多および子宮類線維腫の処置に使用するための組成物
EP2881391A1 (en) 2013-12-05 2015-06-10 Bayer Pharma Aktiengesellschaft Spiroindoline carbocycle derivatives and pharmaceutical compositions thereof
EP3185881B1 (en) 2014-08-26 2022-03-09 Betanien Hospital Methods, agents and compositions for treatment of inflammatory conditions
WO2017221144A1 (en) * 2016-06-20 2017-12-28 Dr. Reddy's Laboratories Limited Process for the preparation of elagolix sodium and its polymorph
WO2018015497A2 (en) 2016-07-21 2018-01-25 ObsEva S.A. Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
BR112019003260B1 (pt) 2016-08-23 2022-07-12 Swan Analytische Instrumente Ag Dispositivo para a eletrodeionização de um líquido de amostra, câmara de tratamento para o uso em um dispositivo e método de eletrodeionização de um lí-quido de amostra para execução em um dispositivo
TWI778979B (zh) 2016-09-30 2022-10-01 瑞士商麥歐文科學有限公司 治療女性不孕症之方法
PL3518933T3 (pl) 2016-09-30 2022-06-20 Myovant Sciences Gmbh Metody leczenia mięśniaków macicy i endometriozy
JP7062673B2 (ja) 2016-09-30 2022-05-06 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
US10821188B2 (en) 2016-12-14 2020-11-03 Purdue Research Foundation Luteinizing hormone-releasing hormone receptor (LHRH-R) conjugates and uses thereof
WO2018189212A1 (en) 2017-04-12 2018-10-18 Sandoz Ag Acid addition salts of an orally available gonadotropin-releasing hormone receptor antagonist
EP3388421B1 (en) 2017-04-13 2019-12-04 Sandoz AG Acid addition salts of an orally available gonadotropin-releasing hormone receptor antagonist
PT3388422T (pt) 2017-04-13 2020-02-18 Sandoz Ag Dispersão sólida amorfa de um antagonista dos recetores de hormonas libertadoras de gonadotrofina disponível por via oral
WO2018198086A1 (en) * 2017-04-28 2018-11-01 Lupin Limited Process for the preparation of elagolix and pharmaceutically acceptable salts thereof
SG11201911598WA (en) 2017-06-05 2020-01-30 ObsEva SA Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis
WO2018224063A2 (en) * 2017-06-08 2018-12-13 Zentiva, K.S. Solid forms of elagolix
US12083227B2 (en) 2017-08-18 2024-09-10 Abbvie Inc. Solid pharmaceutical formulations for treating endometriosis, uterine fibroids, polycystic ovary syndrome or adenomyosis
WO2019036712A1 (en) 2017-08-18 2019-02-21 Abbvie Inc. PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT OF ENDOMETRIOSIS, UTERINE FIBROIDS, POLYKYSTIC OVARY SYNDROME OR ADENOMYOSIS
EA202090461A1 (ru) 2017-08-18 2020-06-29 Эббви Инк. Фармацевтические препараты для лечения эндометриоза, миомы матки, синдрома поликистоза яичников или аденомиоза
CN107935863A (zh) * 2017-11-30 2018-04-20 厦门海乐景生化有限公司 Elagolix的关键原料化合物C的合成方法
CN110938037A (zh) * 2018-09-21 2020-03-31 苏州鹏旭医药科技有限公司 一种依拉戈利钠盐药物中间体的制备方法
WO2019112968A1 (en) 2017-12-05 2019-06-13 Peng Wang Processes to produce elagolix
EP3724167A1 (en) 2017-12-11 2020-10-21 Synthon B.V. Process for preparing elagolix
CN109970663B (zh) * 2017-12-27 2023-04-11 上海科胜药物研发有限公司 一种制备噁拉戈利中间体的方法
CN108129400B (zh) * 2017-12-29 2021-10-15 安帝康（无锡）生物科技有限公司 氘代噁拉戈利衍生物及其用途
EP3781167A4 (en) 2018-04-19 2022-02-23 Abbvie Inc. METHOD OF TREATMENT OF HEAVY MENSTRUAL BLEEDING
CN110669013A (zh) * 2018-07-03 2020-01-10 江苏海悦康医药科技有限公司 一种噁拉戈利中间体的制备方法
BR112021000973A2 (pt) * 2018-07-23 2021-04-20 Abbvie Inc. composições e processos de sódio de elagolix
JP2021532160A (ja) * 2018-08-01 2021-11-25 アッヴィ・インコーポレイテッド エラゴリックスに関する投与計画
EP3572406A1 (en) 2018-10-17 2019-11-27 Sandoz Ag Acid addition salt of elagolix and related compounds
CA3117092A1 (en) 2018-10-29 2020-05-07 ObsEva S.A. Compositions and methods for the treatment of adenomyosis and rectovaginal endometriosis
KR20210100623A (ko) 2018-11-07 2021-08-17 옵스에파 에스에이 에스트로겐-의존성 장애의 치료를 위한 조성물 및 방법
CN109293634A (zh) * 2018-12-04 2019-02-01 中国药科大学 恶拉戈利杂质的制备方法
CN109651171A (zh) * 2019-01-13 2019-04-19 苏州鹏旭医药科技有限公司 依拉戈利及其钠盐的中间体及其盐的制备方法和应用
BR112021013908A2 (pt) 2019-01-15 2021-09-21 Lupin Inc. Composições semelhantes a elagolix deuterado e métodos
CN109761913A (zh) * 2019-02-16 2019-05-17 安徽华胜医药科技有限公司 一种有机金属钯催化合成elagolix中间体的方法
CN109651265A (zh) * 2019-02-16 2019-04-19 安徽诺全药业有限公司 一种Elagolix的制备方法
CN109810065B (zh) * 2019-02-16 2022-07-15 安徽华胜医药科技有限公司 一种恶拉戈利的合成方法
CN110041232A (zh) * 2019-04-10 2019-07-23 丽珠集团新北江制药股份有限公司 一种制备GnRHR药物关键中间体化合物的方法
CN109956906B (zh) * 2019-04-19 2021-01-29 奥锐特药业股份有限公司 一种噁拉戈利关键中间体的制备方法
WO2020240375A1 (en) * 2019-05-24 2020-12-03 Dr. Reddy’S Laboratories Limited Improved process for the preparation of elagolix and its intermediates
CN110204498B (zh) * 2019-06-14 2020-11-27 奥锐特药业股份有限公司 一种高效合成噁拉戈利中间体的方法
CN110372608A (zh) * 2019-07-09 2019-10-25 丽珠集团新北江制药股份有限公司 一种促性腺激素释放激素拮抗剂的制备方法
ES2802815B2 (es) * 2019-07-12 2022-03-14 Moehs Iberica Sl Sal clorhidrato de 3-[2(r)-amino-2-feniletil]-5-(2-fluoro-3-metoxifenil)-1-[2-fluoro-6-(trifluorometil)bencil]-6-metil-1h-pirimidin-2,4(1h,3h)-diona (i) en forma solida, procedimiento para su preparacion y uso de la misma en la sintesis de elagolix
CN110372609B (zh) * 2019-07-25 2021-04-09 奥锐特药业股份有限公司 一种噁拉戈利钠盐的纯化方法
WO2021016929A1 (zh) * 2019-07-31 2021-02-04 深圳仁泰医药科技有限公司 恶拉戈利与乙胺嘧啶的共晶型a及其制备方法和用途
KR20220045198A (ko) 2019-08-08 2022-04-12 옵스에파 에스에이 에스트로겐-의존성 장애의 치료를 위한 gnrh 길항제
CA3148939A1 (en) 2019-08-08 2021-02-11 ObsEva S.A. Compositions and methods for the treatment of estrogen-dependent disorders
CN114667141A (zh) 2019-09-03 2022-06-24 奥布赛瓦股份公司 用于促进胚胎移植和预防流产的催产素拮抗剂给药方案
IT201900015458A1 (it) 2019-09-03 2021-03-03 Ind Chimica Srl Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo
IT202000001390A1 (it) 2020-01-24 2021-07-24 Ind Chimica Srl Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo
WO2021044230A1 (en) * 2019-09-03 2021-03-11 Industriale Chimica S.R.L. Process for the synthesis of the sodium salt of 4-[[(lr)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)-phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-l(2h)-pyrimidinyl]-l- phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process
TWI755055B (zh) * 2019-09-18 2022-02-11 台灣神隆股份有限公司 用於製備惡拉戈利鈉及其中間體的方法
WO2021064561A1 (en) * 2019-10-03 2021-04-08 Neuland Laboratories Limited An improved process for the preparation of elagolix sodium
CN112694445B (zh) * 2019-10-22 2023-07-28 成都倍特药业股份有限公司 一种噁拉戈利钠中间体的纯化方法
ES2822398B2 (es) 2019-10-30 2022-03-02 Moehs Iberica Sl 3-((R)-2-(Amino-2-feniletil)-1-(2-fluoro-6-trifluorometilbencil)-5-yodo-6-metil-1H-pirimidin-2,4-diona o una sal de la misma, procedimiento para su preparación y su uso en la síntesis de elagolix
WO2021130776A1 (en) * 2019-12-27 2021-07-01 Msn Laboratories Private Limited, R&D Center An improved process for the preparation of 4-({(1 r)-2-[5-(2-fluoro-3methoxyphenyl)-3-{[2-fluoro-6-(trifluoro methyl) phenyl]methyl}-4-methyl-2,6-dioxo-3,6dihydropyrimidin-1(2 h)-yl]-1-phenylethyl}amino)butanoic acid or its pharmaceutically acceptable salts
CN113125575B (zh) * 2019-12-31 2023-04-18 济南尚博生物科技有限公司 一种1-(2-氟-6-(三氟甲基)苄基)-6-甲基嘧啶-二酮的定量分析方法
CN111116490A (zh) * 2020-01-15 2020-05-08 奥锐特药业股份有限公司 一种噁拉戈利中间体水杨酸盐的制备与纯化方法
US20230102503A1 (en) 2020-02-10 2023-03-30 ObsEva S.A. Biomarkers for oxytocin receptor antagonist therapy
EP4114396A4 (en) * 2020-03-05 2024-04-10 Abbvie Inc. METHOD OF ADMINISTRATION OF ELAGOLIX
WO2021180862A1 (en) 2020-03-12 2021-09-16 Synthon B.V. Pharmaceutical compositions comprising elagolix sodium
CN111333548B (zh) * 2020-04-10 2022-04-26 江苏海悦康医药科技有限公司 1-(2-氟-6-(三氟甲基)苄基)脲的制备方法
CN113527213B (zh) * 2020-04-20 2023-01-03 上海英诺富成生物科技有限公司 促性激素释放激素受体拮抗剂及其用途
CN113683572A (zh) * 2020-05-18 2021-11-23 陈晓雯 噁拉戈利的中间体及其制备方法和应用
CN112457258A (zh) * 2020-11-26 2021-03-09 诚达药业股份有限公司 一种噁拉戈利钠及其中间体的制备方法
EP4284374A1 (en) 2021-01-29 2023-12-06 Abbvie Inc. Methods of administrating elagolix
KR102656087B1 (ko) 2024-01-12 2024-04-09 주식회사 씨엠지 Led 소자의 에폭시 수지 코팅층 형성 방법

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1072219C (zh) 1995-06-01 2001-10-03 武田药品工业株式会社 二氮杂䓬酮、其生产和用途
CA2229205A1 (en) 1995-10-19 1997-04-24 Shuichi Furuya Thienopyridine derivatives, their productions and use
DE69623655T2 (de) 1995-10-19 2003-04-24 Takeda Chemical Industries, Ltd. Chinolinderivate als gnrh antagonisten
NZ325060A (en) 1995-12-14 2000-02-28 Merck & Co Inc Non peptide indole derivative and their use as antagonists of gonadotropin releasing hormone
SK77598A3 (en) 1995-12-14 1999-01-11 Merck & Co Inc Nonpeptide derivatives, pharmaceutical composition containing them and their use
IL124459A0 (en) * 1995-12-14 1998-12-06 Merck & Co Inc Antagonists of gonadotropin releasing hormone
JP3092947B2 (ja) 1995-12-14 2000-09-25 メルク エンド カンパニー インコーポレーテッド ゴナドトロピン放出ホルモン拮抗剤
AU729663B2 (en) 1997-06-05 2001-02-08 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
CA2292605A1 (en) 1997-06-05 1998-12-10 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
CA2291829A1 (en) 1997-06-05 1998-12-10 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
JP2002502427A (ja) 1997-06-05 2002-01-22 メルク エンド カンパニー インコーポレーテッド ゴナドトロピン放出ホルモンの拮抗薬
US6313301B1 (en) 1997-08-13 2001-11-06 Takeda Chemical Industries, Ltd. Thienopyridine derivatives, their intermediates and production thereof
EP1185530A1 (en) 1999-05-14 2002-03-13 Neurocrine Biosciences, Inc. Imidazo- and pyrrolo[1,2-a]pyrimid-4-ones as gonadotropin-releasing hormone receptor antagonists
US20020065309A1 (en) 1999-08-04 2002-05-30 Ge Peng Novel Bicyclic and tricyclic pyrrolidine derivatives as GnRH antagonists
KR20020045609A (ko) 1999-10-15 2002-06-19 추후기재 고나도트로핀-분비 호르몬 수용체 길항제 및 이와 관련된방법
JP4931314B2 (ja) 2000-01-25 2012-05-16 ニューロクライン バイオサイエンシーズ，インコーポレイテッド 性腺刺激ホルモン放出ホルモンレセプタアンタゴニストおよびそれに関連した方法
SE0100566D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
JP2005505525A (ja) 2001-08-02 2005-02-24 ニューロクライン バイオサイエンシーズ， インコーポレイテッド 性腺刺激ホルモン放出ホルモンレセプターアンタゴニストおよびそれに関連する方法
EP1411941A2 (en) 2001-08-02 2004-04-28 Neurocrine Biosciences, Inc. Pyridinone and pyridazinone derivatives as gonadotropin-releasing hormone receptor antagonists
EP1412363A1 (en) 2001-08-02 2004-04-28 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists
MXPA04000986A (es) 2001-08-02 2005-02-17 Neurocrine Biosciences Inc 1,2,3-triazin-3,5-dionas sustituidas como antagonistas del receptor de hormona de liberacion de gonadotropina (gnrh).
AU2002324586B2 (en) 2001-08-02 2008-04-24 Neurocrine Biosciences, Inc. 1,3,5-triazine-2,4,6-triones, preparation and use as gonadotropin-releasing hormone receptor antagonists
CN100376246C (zh) 2003-07-07 2008-03-26 纽罗克里生物科学有限公司 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物
CN100424078C (zh) * 2003-07-07 2008-10-08 纽罗克里生物科学有限公司 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物
WO2005007633A1 (en) 2003-07-07 2005-01-27 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

Also Published As

Publication number Publication date
SI1646389T1 (sl) 2009-02-28
HRP20080646T3 (en) 2009-01-31
KR20060031851A (ko) 2006-04-13
BRPI0412314A (pt) 2006-08-22
CY1108656T1 (el) 2014-04-09
IL172833A0 (en) 2006-06-11
DE602004016516D1 (de) 2008-10-23
EP1646389B1 (en) 2008-09-10
CN1819829A (zh) 2006-08-16
US7056927B2 (en) 2006-06-06
US7176211B2 (en) 2007-02-13
KR101139148B1 (ko) 2012-04-26
PT1646389E (pt) 2008-12-19
US20070191403A1 (en) 2007-08-16
BRPI0412314B8 (pt) 2021-05-25
AU2004257639A1 (en) 2005-01-27
CN100424078C (zh) 2008-10-08
JP5226760B2 (ja) 2013-07-03
US7419983B2 (en) 2008-09-02
PL1646389T3 (pl) 2009-03-31
IL172833A (en) 2011-03-31
EA010370B1 (ru) 2008-08-29
ATE407679T1 (de) 2008-09-15
NO334897B1 (no) 2014-06-30
BRPI0412314B1 (pt) 2019-03-06
MXPA06000297A (es) 2006-03-28
US20060122202A1 (en) 2006-06-08
AU2004257639B2 (en) 2011-01-06
EA200600190A1 (ru) 2006-08-25
EP1646389A1 (en) 2006-04-19
ES2314448T3 (es) 2009-03-16
US20050038057A1 (en) 2005-02-17
CA2531508A1 (en) 2005-01-27
JP4722844B2 (ja) 2011-07-13
ZA200600475B (en) 2007-04-25
WO2005007165A1 (en) 2005-01-27
NZ544747A (en) 2009-06-26
DK1646389T3 (da) 2009-01-05
JP2011088902A (ja) 2011-05-06
CA2531508C (en) 2013-10-08
JP2007521309A (ja) 2007-08-02

Similar Documents

Publication Publication Date Title
NO20056251L (no) Pyrimidin-2,4-dionderivater som gonadotropin-frigjorende hormon reseptor antagonist
IL172834A0 (en) Pyrimidine-,2,4-dione derivatives and pharmaceutical compositions containing the same
PT1678166E (pt) Inibidores de proteína-quinase
MX2007013624A (es) Inhibidores de proteina cinasa.
MY134848A (en) Pyrrolo[2,1-f] [1,2,4] triazine inhibitors of kinases
DE602004007239D1 (de) 4-AMINOTHIENOÄ2,3-dÜ PYRIMIDIN -6-CARBONITRIL-DERIVATIVE ZUR VERWENDUNG ALS PDE7 INHIBITOREN
MX2007014619A (es) Pirrolopiridinas de utilidad como inhibidores de proteina quinasa.
MX2023013582A (es) Regimenes de dosificacion de antagonista de hormona liberadora de gonadotropina para tratar miomas uterinos y reducir la menstruacion.
TW200613306A (en) Imidazotriazines as protein kinase inhibitors
EA200600811A1 (ru) НОВЫЕ ПРОИЗВОДНЫЕ ТЕТРАГИДРОСПИРО {ПИПЕРИДИН-2,7'-ПИРРОЛО [3,2-b]ПИРИДИНА} И НОВЫЕ ПРОИЗВОДНЫЕ ИНДОЛА, ПРИМЕНЕНИЕ ДЛЯ ЛЕЧЕНИЯ РАССТРОЙСТВ, СВЯЗАННЫХ С 5-HT-РЕЦЕПТОРОМ
IL174678A0 (en) Arylindenophyridines and arylindenophyrimidines and their use as adenosine a2a receptor antagonist
WO2003011293A3 (en) Pyridinone and pyridazinone derivatives as gonadotropin-releasing hormone receptor antagonists
MX2021011389A (es) Compuestos de imidazolonilquinolina y usos terapeuticos de los mismos.
MX2021006012A (es) Derivados de amino triazolo quinazolina 7-, 8-, y 10-sustituidos como antagonistas de receptor de adenosina, composiciones farmaceuticas y su uso.
NO20040500L (no) 1, 3, 5-triazin-2, 4, 6-trioner, fremstilling og anvendelse som gonadotropin-frigjorende hormon reseptor antagonister
EA202190322A1 (ru) ИМИДАЗО[1,2-b]ПИРИДАЗИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ TRK
BRPI0414778A (pt) 6-aril-7-halo-imidazo[1,2-a]pirimidinas como agentes anticáncer
TW200508236A (en) Pyrazolo[1,5-a]pyrimidine derivatives