BRPI0514096A - processo para a preparação de derivados-2-substituìdos de estrona e estradiol, composto, e, processo para a preparação do mesmo - Google Patents

processo para a preparação de derivados-2-substituìdos de estrona e estradiol, composto, e, processo para a preparação do mesmo

Info

Publication number
BRPI0514096A
BRPI0514096A BRPI0514096-0A BRPI0514096A BRPI0514096A BR PI0514096 A BRPI0514096 A BR PI0514096A BR PI0514096 A BRPI0514096 A BR PI0514096A BR PI0514096 A BRPI0514096 A BR PI0514096A
Authority
BR
Brazil
Prior art keywords
compound
preparation
formula
estrone
estradiol
Prior art date
Application number
BRPI0514096-0A
Other languages
English (en)
Inventor
Johannes Stoelwinder
Nicolaas Elisabeth Corne Moers
Original Assignee
Organon Nv
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 Organon Nv filed Critical Organon Nv
Publication of BRPI0514096A publication Critical patent/BRPI0514096A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J75/00—Processes for the preparation of steroids in general
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J75/00—Processes for the preparation of steroids in general
    • C07J75/005—Preparation of steroids by cyclization of non-steroid compounds
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Pyrane Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

PROCESSO PARA A PREPARAçãO DE DERIVADOS-2-SUBSTITUìDOS DE ESTRONA E ESTRADIOL, COMPOSTO, E, PROCESSO PARA A PREPARAçãO DO MESMO A invenção fornece um processo para a preparação de derivados 2-substituídos de estrona e estradiol, compreendendo i) a preparação de um composto de fórmula geral (II), pela reação de um composto de fórmula geral (I) em uma ou mais etapas, com um composto de fórmula geral II em que R1 é um grupo C~ 1~-C~ 10~ alquila, alquenila ou arila; -C1, -Br, -I, -F; -CN; -OH; ou um grupo -OR2, -O(CO)R2 ou -R2-OH, em que R2 é um grupo alquila ou alquileno, tendo 1 - 6 átomos C; e a ligação entre os átomos 9 e 10 é uma única ou uma dupla ligação. ii) aromatização do composto de fórmula geral II com um composto de fórmula geral III em que R1 e R2 têm os significados definidos acima; e iii) opcionalmente, redução do composto de fórmula geral III a um composto de fórmula geral IV, em que R1 e R2 têm os significados definidos acima. Além disso, a invenção fornece diversos compostos novos, que podem ser intermediários no processo acima e processos para preparar estes novos compostos. A invenção também fornece 2-alcóxi-estrona, 2-alcóxi-estradiol ou suas misturas, essencialmente livres de outros intermediários estrogênicos.
BRPI0514096-0A 2004-08-04 2005-08-01 processo para a preparação de derivados-2-substituìdos de estrona e estradiol, composto, e, processo para a preparação do mesmo BRPI0514096A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP04103742 2004-08-04
PCT/EP2005/053732 WO2006013196A1 (en) 2004-08-04 2005-08-01 Process for the preparation 2-substituted-derivatives of estrone and estradiol

Publications (1)

Publication Number Publication Date
BRPI0514096A true BRPI0514096A (pt) 2008-05-27

Family

ID=34929415

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0514096-0A BRPI0514096A (pt) 2004-08-04 2005-08-01 processo para a preparação de derivados-2-substituìdos de estrona e estradiol, composto, e, processo para a preparação do mesmo

Country Status (20)

Country Link
US (2) US7910756B2 (pt)
EP (1) EP1776378B1 (pt)
JP (1) JP5075626B2 (pt)
KR (1) KR20070040386A (pt)
CN (1) CN1993376A (pt)
AR (1) AR050195A1 (pt)
AT (1) ATE447580T1 (pt)
AU (1) AU2005268768B2 (pt)
BR (1) BRPI0514096A (pt)
CA (1) CA2573133C (pt)
DE (1) DE602005017500D1 (pt)
EC (1) ECSP077228A (pt)
ES (1) ES2334244T3 (pt)
IL (1) IL180381A0 (pt)
MX (1) MX2007001340A (pt)
NO (1) NO20070747L (pt)
RU (1) RU2007107914A (pt)
TW (1) TW200611909A (pt)
WO (1) WO2006013196A1 (pt)
ZA (1) ZA200700483B (pt)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ2008275A3 (cs) 2008-05-05 2009-05-06 Prírodovedecká Fakulta Uk Ligandy estrogenových receptoru alfa a beta, zpusob jejich prípravy a farmaceutické prostredky, které je obsahují
WO2012020417A1 (en) 2010-08-10 2012-02-16 Reliance Life Sciences Pvt. Ltd. Process for the preparation of estradiol and its derivatives
WO2013025532A2 (en) * 2011-08-12 2013-02-21 Siemens Healthcare Diagnostics Inc. Detection of sex steroids
CN104592339A (zh) * 2014-12-30 2015-05-06 湖南新合新生物医药有限公司 雌甾-4,9-二烯-3,17-二酮的制备方法
CN104497088B (zh) * 2014-12-30 2016-08-24 湖南新合新生物医药有限公司 19-去甲-4-雄甾烯-3,17-二酮的制备方法
ITUB20155260A1 (it) * 2015-10-30 2017-04-30 Ind Chimica Srl PROCESSO PER LA PREPARAZIONE DI 17?-idrossi-des-A-androst-9,10-en-5-one
CN108003210A (zh) * 2018-01-24 2018-05-08 四川理工学院 一种雌甾-4,9-二烯-3,17-二酮的制备方法
CN108997463B (zh) * 2018-08-09 2021-05-14 四川理工学院 一种雌甾-4，9-二烯-3，17-二酮制备方法
CN112409434B (zh) * 2020-11-27 2021-10-26 厦门欧瑞捷生物科技有限公司 一种去氢孕酮的合成方法
CN113861158B (zh) * 2021-11-22 2023-02-10 湖南新合新生物医药有限公司 一种合成甲基双烯双酮关键中间体的方法
CN114853802B (zh) * 2022-03-22 2023-11-28 河北康泰药业有限公司 一种谷内酯衍生物及其制备方法、药物组合物和应用

Family Cites Families (15)

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US2997488A (en) * 1959-06-20 1961-08-22 Organon 2-methyl-19-nor-steroids
FR1468608A (fr) * 1960-08-04 1967-02-10 Upjohn Co 2-alpha-fluoro stéroïdes de la série de la 19-norandrostène et leur procédé d'obtention
FR1368721A (fr) * 1961-04-14 1964-08-07 Roussel Uclaf Dérivés de la 19-nor testostérone et procédé de préparation
BE616293A (fr) * 1961-04-14 1962-10-11 Roussel Uclaf Dérivés de la 19-nor testostérone et procédé de préparation
US3519714A (en) * 1966-03-15 1970-07-07 Herchel Smith Synthesis of gona-1,3,5(10)-trienes
US4400524A (en) 1981-07-28 1983-08-23 The Upjohn Company Grignard reagents prepared from 5-halopentan-2-one propylene ketals
DE3208432A1 (de) * 1982-03-09 1983-09-15 The Upjohn Co., 49001 Kalamazoo, Mich. Verfahren zur herstellung von 19-norandrostendion, zwischenprodukt des 19-norandrostendions und verfahren zu seiner herstellung
US5504074A (en) * 1993-08-06 1996-04-02 Children's Medical Center Corporation Estrogenic compounds as anti-angiogenic agents
US5521168A (en) * 1994-10-13 1996-05-28 Alcon Laboratories, Inc. Estrogen metabolites for lowering intraocular pressure
US5998639A (en) * 1995-11-06 1999-12-07 Akzo Nobel, N.V. Sulfatation of estrogen mixtures
IL119649A (en) * 1995-11-30 2002-03-10 Akzo Nobel Nv Preparation of Cyclic Kills of History - 3 keto- (5) 10, (-9) 11 steroidadians
US6051726A (en) * 1997-03-13 2000-04-18 Pharm-Eco Laboratories, Inc. Synthesis of 2-alkoxyestradiols
US7087592B1 (en) * 1999-08-23 2006-08-08 Entre Med, Inc. Compositions comprising purified 2-methoxyestradiol and methods of producing same
WO2001014405A2 (en) 1999-08-23 2001-03-01 Entremed, Inc. Methods of obtaining 2-methoxyestradiol of high purity
AU8838601A (en) 2000-11-27 2002-06-03 Entremed Inc Antiangiogenic agents

Also Published As

Publication number Publication date
AU2005268768A1 (en) 2006-02-09
ZA200700483B (en) 2008-09-25
US20110152544A1 (en) 2011-06-23
EP1776378A1 (en) 2007-04-25
RU2007107914A (ru) 2008-09-10
NO20070747L (no) 2007-04-23
KR20070040386A (ko) 2007-04-16
AU2005268768B2 (en) 2011-10-13
ES2334244T3 (es) 2010-03-08
JP5075626B2 (ja) 2012-11-21
US20090012319A1 (en) 2009-01-08
ECSP077228A (es) 2007-03-29
CA2573133A1 (en) 2006-02-09
MX2007001340A (es) 2007-03-27
US7910756B2 (en) 2011-03-22
ATE447580T1 (de) 2009-11-15
CA2573133C (en) 2012-07-10
WO2006013196A1 (en) 2006-02-09
EP1776378B1 (en) 2009-11-04
IL180381A0 (en) 2007-06-03
CN1993376A (zh) 2007-07-04
JP2008509109A (ja) 2008-03-27
AR050195A1 (es) 2006-10-04
TW200611909A (en) 2006-04-16
DE602005017500D1 (de) 2009-12-17

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Legal Events

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

Free format text: REFERENTE AS 5A E 6A 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 2158 DE 15/05/2012.