ATE407679T1 - Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten - Google Patents

Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten

Info

Publication number
ATE407679T1
ATE407679T1 AT04777603T AT04777603T ATE407679T1 AT E407679 T1 ATE407679 T1 AT E407679T1 AT 04777603 T AT04777603 T AT 04777603T AT 04777603 T AT04777603 T AT 04777603T AT E407679 T1 ATE407679 T1 AT E407679T1
Authority
AT
Austria
Prior art keywords
sub
receptor antagonists
gonadotropin
releasing hormone
pyrimidine
Prior art date
Application number
AT04777603T
Other languages
English (en)
Inventor
Zhiqiang Guo
Yongsheng Chen
Dongpei Wu
Chen Chen
Warren Wade
Wesley Dwight
Charles Huang
Fabio Tucci
Original Assignee
Neurocrine Biosciences Inc
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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=ATE407679(T1) "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
Application granted granted Critical
Publication of ATE407679T1 publication Critical patent/ATE407679T1/de

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A61P5/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Anesthesiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (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)
AT04777603T 2003-07-07 2004-07-06 Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten ATE407679T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US48543403P 2003-07-07 2003-07-07

Publications (1)

Publication Number Publication Date
ATE407679T1 true ATE407679T1 (de) 2008-09-15

Family

ID=34079121

Family Applications (1)

Application Number Title Priority Date Filing Date
AT04777603T ATE407679T1 (de) 2003-07-07 2004-07-06 Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten

Country Status (24)

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

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US12083227B2 (en) 2017-08-18 2024-09-10 Abbvie Inc. Solid pharmaceutical formulations for treating endometriosis, uterine fibroids, polycystic ovary syndrome or adenomyosis
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
JP7200261B2 (ja) * 2017-12-05 2023-01-06 スージョウ ポンシュー ファーマテック カンパニー リミテッド エラゴリクスを作製するプロセス
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
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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
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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
CN112469417A (zh) * 2018-07-23 2021-03-09 艾伯维公司 恶拉戈利钠组合物和方法
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
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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
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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
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
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
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
US20220242831A1 (en) * 2019-05-24 2022-08-04 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
CN112672998B (zh) 2019-07-31 2022-06-21 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
KR20220061120A (ko) 2019-08-08 2022-05-12 옵스에파 에스에이 에스트로겐-의존성 장애 치료용 조성물 및 방법
US20220288154A1 (en) 2019-08-08 2022-09-15 ObsEva S.A. Gnrh antagonists for the treatment of estrogen-dependent disorders
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