CN100424078C - 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 - Google Patents

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 Download PDF

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Publication number
CN100424078C
CN100424078C CNB2004800195023A CN200480019502A CN100424078C CN 100424078 C CN100424078 C CN 100424078C CN B2004800195023 A CNB2004800195023 A CN B2004800195023A CN 200480019502 A CN200480019502 A CN 200480019502A CN 100424078 C CN100424078 C CN 100424078C
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compound
fluoro
pyrimidine
amino
trifluoromethyl
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CN1819829A (zh
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郭志强
陈永胜
吴东培
陈晨
沃伦·韦德
韦斯利·J·德怀特
查尔斯·Q·黄
法维奥·C·图奇
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Neurocrine Biosciences Inc
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Neurocrine Biosciences Inc
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    • 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
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    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (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)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Anesthesiology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (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)
CNB2004800195023A 2003-07-07 2004-07-06 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 Expired - Lifetime CN100424078C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US48543403P 2003-07-07 2003-07-07
US60/485,434 2003-07-07

Publications (2)

Publication Number Publication Date
CN1819829A CN1819829A (zh) 2006-08-16
CN100424078C true CN100424078C (zh) 2008-10-08

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

Cited By (4)

* Cited by examiner, † Cited by third party
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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
WO2019128983A1 (zh) 2017-12-27 2019-07-04 浙江华海药业股份有限公司 一种制备噁拉戈利中间体的方法及其组合物
CN110372609A (zh) * 2019-07-25 2019-10-25 奥锐特药业股份有限公司 一种噁拉戈利钠盐的纯化方法
US12268689B2 (en) 2019-07-31 2025-04-08 Shenzhen Jingtai Technology Co., Ltd Eutectic form A of Elagolix and pyrimethamine, preparation method therefor and use thereof

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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
ATE428427T1 (de) 2003-07-07 2009-05-15 Neurocrine Biosciences Inc Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten
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MX2009010828A (es) 2007-04-06 2009-10-29 Neurocrine Biosciences Inc Antagonistas del receptor de la hormona liberadora de gonadotropina y metodos relacionados con los mismos.
PA8775701A1 (es) 2007-04-06 2009-04-23 Neurocrine Biosciences Inc Antagonista de los receptores de la hormona liberadora de gonadotropina y procedimientos relacionados con ellos
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JP5757956B2 (ja) * 2009-11-20 2015-08-05 エスケー ケミカルス シーオー．， エルティーディー．Ｓｋ Ｃｈｅｍｉｃａｌｓ Ｃｏ．， Ｌｔｄ． ゴナドトロピン放出ホルモン受容体拮抗剤、その製造方法及びそれを含む医薬組成物
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
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WO2017221144A1 (en) * 2016-06-20 2017-12-28 Dr. Reddy's Laboratories Limited Process for the preparation of elagolix sodium and its polymorph
CN115569132A (zh) 2016-07-21 2023-01-06 奥布赛瓦股份公司 促进胚胎植入和预防流产的催产素拮抗剂给药方案
JP6843230B2 (ja) 2016-08-23 2021-03-17 スワン・アナリティスク・インストゥルメント・アーゲー 液体の電気脱イオン化のための装置および方法
SI3518933T2 (sl) 2016-09-30 2025-05-30 Sumitomo Pharma Switzerland Gmbh Metode zdravljenja materničnih miom in endometrioze
MA46353A (fr) 2016-09-30 2019-08-07 Myovant Sciences Gmbh Méthodes de traitement de l'infertilité féminine
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EP3388421B1 (en) 2017-04-13 2019-12-04 Sandoz AG Acid addition salts of an orally available gonadotropin-releasing hormone receptor antagonist
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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
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