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 mesmoInfo
- 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
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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Reproductive Health (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Vascular Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
- Pyrane Compounds (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.
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)
| 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 |
| EP2742352B1 (en) * | 2011-08-12 | 2018-02-28 | 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CH409944A (fr) | 1961-04-14 | 1966-03-31 | Roussel Uclaf | Procédé de préparation de dérivés de la 19-nor-testostérone |
| 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 |
| JP5317381B2 (ja) | 1999-08-23 | 2013-10-16 | エントレメッド インコーポレイテッド | 高純度２−メトキシエストラジオールの生成方法 |
| AU8838601A (en) | 2000-11-27 | 2002-06-03 | Entremed Inc | Antiangiogenic agents |
-
2005
- 2005-07-14 TW TW094123942A patent/TW200611909A/zh unknown
- 2005-08-01 ES ES05767940T patent/ES2334244T3/es active Active
- 2005-08-01 RU RU2007107914/04A patent/RU2007107914A/ru not_active Application Discontinuation
- 2005-08-01 JP JP2007524335A patent/JP5075626B2/ja not_active Expired - Fee Related
- 2005-08-01 WO PCT/EP2005/053732 patent/WO2006013196A1/en active Application Filing
- 2005-08-01 DE DE602005017500T patent/DE602005017500D1/de active Active
- 2005-08-01 EP EP05767940A patent/EP1776378B1/en active Active
- 2005-08-01 BR BRPI0514096-0A patent/BRPI0514096A/pt not_active IP Right Cessation
- 2005-08-01 CA CA2573133A patent/CA2573133C/en not_active Expired - Fee Related
- 2005-08-01 AU AU2005268768A patent/AU2005268768B2/en not_active Ceased
- 2005-08-01 MX MX2007001340A patent/MX2007001340A/es active IP Right Grant
- 2005-08-01 AT AT05767940T patent/ATE447580T1/de not_active IP Right Cessation
- 2005-08-01 KR KR1020077002976A patent/KR20070040386A/ko not_active Application Discontinuation
- 2005-08-01 US US11/659,147 patent/US7910756B2/en not_active Expired - Fee Related
- 2005-08-01 CN CNA2005800261640A patent/CN1993376A/zh active Pending
- 2005-08-04 AR ARP050103233A patent/AR050195A1/es unknown
-
2006
- 2006-12-27 IL IL180381A patent/IL180381A0/en unknown
-
2007
- 2007-01-16 ZA ZA200700483A patent/ZA200700483B/xx unknown
- 2007-02-05 EC EC2007007228A patent/ECSP077228A/es unknown
- 2007-02-08 NO NO20070747A patent/NO20070747L/no not_active Application Discontinuation
-
2011
- 2011-02-22 US US13/031,975 patent/US20110152544A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US7910756B2 (en) | 2011-03-22 |
| IL180381A0 (en) | 2007-06-03 |
| ZA200700483B (en) | 2008-09-25 |
| ATE447580T1 (de) | 2009-11-15 |
| WO2006013196A1 (en) | 2006-02-09 |
| CN1993376A (zh) | 2007-07-04 |
| CA2573133A1 (en) | 2006-02-09 |
| RU2007107914A (ru) | 2008-09-10 |
| JP5075626B2 (ja) | 2012-11-21 |
| EP1776378B1 (en) | 2009-11-04 |
| US20110152544A1 (en) | 2011-06-23 |
| MX2007001340A (es) | 2007-03-27 |
| ES2334244T3 (es) | 2010-03-08 |
| AR050195A1 (es) | 2006-10-04 |
| KR20070040386A (ko) | 2007-04-16 |
| CA2573133C (en) | 2012-07-10 |
| DE602005017500D1 (de) | 2009-12-17 |
| JP2008509109A (ja) | 2008-03-27 |
| AU2005268768A1 (en) | 2006-02-09 |
| TW200611909A (en) | 2006-04-16 |
| ECSP077228A (es) | 2007-03-29 |
| AU2005268768B2 (en) | 2011-10-13 |
| NO20070747L (no) | 2007-04-23 |
| US20090012319A1 (en) | 2009-01-08 |
| EP1776378A1 (en) | 2007-04-25 |
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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. |