BRPI0412327A - derivados de pirimidina-2,4-diona como antagonistas de receptor de hormÈnio liberador de gonadotropina - Google Patents

derivados de pirimidina-2,4-diona como antagonistas de receptor de hormÈnio liberador de gonadotropina

Info

Publication number
BRPI0412327A
BRPI0412327A BRPI0412327-1A BRPI0412327A BRPI0412327A BR PI0412327 A BRPI0412327 A BR PI0412327A BR PI0412327 A BRPI0412327 A BR PI0412327A BR PI0412327 A BRPI0412327 A BR PI0412327A
Authority
BR
Brazil
Prior art keywords
sub
receptor antagonists
releasing hormone
pyrimidine
hormone receptor
Prior art date
Application number
BRPI0412327-1A
Other languages
English (en)
Inventor
Yun-Fei Zhu
Collin Regan
Jaime K Rueter
Zhiqiang Guo
Yongsheng Chen
Charles Q Huang
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
Application filed by Neurocrine Biosciences Inc filed Critical Neurocrine Biosciences Inc
Publication of BRPI0412327A publication Critical patent/BRPI0412327A/pt

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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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Anesthesiology (AREA)
  • Dermatology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"DERIVADOS DE PIRIMIDINA-2,4-DIONA COMO ANTAGONISTAS DE RECEPTOR DE HORMÈNIO LIBERADOR DE GONADOTROPINA". São descritos antagonistas de receptor de GnRH, os quais têm utilidade no tratamento de uma variedade de condições relacionadas a hormónios sexuais, tanto em homens como em mulheres. Os compostos dessa invenção têm a fórmula estrutural (I) , em que R~ 1a~, R~ 1b~, R~ 2a~, R~ 2b~, R~ 3~, R~ 4~, R~ 5~, R~ 6~, R~ 7~ e X são como definidos aqui, incluindo estereoisómeros, pró-drogas e sais farmaceuticamente aceitáveis destes. São também descritas composições contendo um composto dessa invenção em combinação com um veículo farmaceuticamente aceitável, bem como métodos relacionados ao uso das mesmas para antagonizar hormónio liberador de gonadotropina em um paciente que necessite destes.
BRPI0412327-1A 2003-07-07 2004-07-06 derivados de pirimidina-2,4-diona como antagonistas de receptor de hormÈnio liberador de gonadotropina BRPI0412327A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US48543603P 2003-07-07 2003-07-07
PCT/US2004/021569 WO2005007164A1 (en) 2003-07-07 2004-07-06 Pyrimidine-2,4-dione derivatives as gonadotropin-releasing hormone receptor antagonists

Publications (1)

Publication Number Publication Date
BRPI0412327A true BRPI0412327A (pt) 2006-09-05

Family

ID=34079122

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0412327-1A BRPI0412327A (pt) 2003-07-07 2004-07-06 derivados de pirimidina-2,4-diona como antagonistas de receptor de hormÈnio liberador de gonadotropina

Country Status (14)

Country Link
US (2) US7071200B2 (pt)
EP (1) EP1660091B1 (pt)
JP (2) JP4658044B2 (pt)
KR (1) KR20060052790A (pt)
CN (2) CN100376246C (pt)
AT (1) ATE428427T1 (pt)
AU (1) AU2004257636B2 (pt)
BR (1) BRPI0412327A (pt)
CA (1) CA2531507C (pt)
DE (1) DE602004020638D1 (pt)
EA (1) EA200600188A1 (pt)
IL (1) IL172834A0 (pt)
MX (1) MXPA06000300A (pt)
WO (1) WO2005007164A1 (pt)

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EP1644342B1 (en) * 2003-07-07 2012-05-09 Neurocrine Biosciences, Inc. Arylpyrimidines useful for the treatment of sex hormone-related conditions such as endometriosis, prostate cancer and the like
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WO2019115019A1 (en) * 2017-12-11 2019-06-20 Synthon B.V. Process for preparing elagolix
CN112469417A (zh) 2018-07-23 2021-03-09 艾伯维公司 恶拉戈利钠组合物和方法
US20220242831A1 (en) * 2019-05-24 2022-08-04 Dr. Reddy's Laboratories Limited Improved process for the preparation of elagolix and its intermediates
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
CN112300081A (zh) * 2019-07-31 2021-02-02 上海度德医药科技有限公司 噁拉戈利的中间体及其制备方法和应用
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
CN110938038A (zh) * 2019-11-14 2020-03-31 上海星酶生物科技有限公司 一种c13h10f4n2o2的制备工艺
CN111333586A (zh) * 2020-02-19 2020-06-26 诚达药业股份有限公司 一种含有6-甲基尿嘧啶结构化合物的制备方法
CN111333587B (zh) * 2020-04-11 2023-04-07 东莞市东阳光新药研发有限公司 取代的嘧啶-2,4(1h,3h)-二酮衍生物及其用途
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
CN111574461A (zh) * 2020-05-29 2020-08-25 奥锐特药业股份有限公司 一种噁拉戈利中间体的成盐纯化方法及获得的噁拉戈利中间体精品

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Also Published As

Publication number Publication date
CA2531507A1 (en) 2005-01-27
AU2004257636A1 (en) 2005-01-27
EP1660091A1 (en) 2006-05-31
US7329669B2 (en) 2008-02-12
JP2007521308A (ja) 2007-08-02
CN100376246C (zh) 2008-03-26
AU2004257636B2 (en) 2011-01-06
EP1660091B1 (en) 2009-04-15
DE602004020638D1 (de) 2009-05-28
EA200600188A1 (ru) 2006-08-25
KR20060052790A (ko) 2006-05-19
CN1826119A (zh) 2006-08-30
MXPA06000300A (es) 2006-03-28
JP2011088903A (ja) 2011-05-06
CA2531507C (en) 2013-10-01
JP4658044B2 (ja) 2011-03-23
ATE428427T1 (de) 2009-05-15
US20070015778A1 (en) 2007-01-18
WO2005007164A1 (en) 2005-01-27
US7071200B2 (en) 2006-07-04
IL172834A0 (en) 2006-06-11
US20050043338A1 (en) 2005-02-24
CN101229165A (zh) 2008-07-30

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE AS 6A, 7A E 8A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2159 DE 22/05/2012.