BR9807079A - Composto de derivado de 16-hidróxi-11- (fenil substituìdo) - estra-4,9-dieno, uso de um composto, formulação farmacêutica, e processo para a preparação de um composto. - Google Patents
Composto de derivado de 16-hidróxi-11- (fenil substituìdo) - estra-4,9-dieno, uso de um composto, formulação farmacêutica, e processo para a preparação de um composto.Info
- Publication number
- BR9807079A BR9807079A BR9807079-7A BR9807079A BR9807079A BR 9807079 A BR9807079 A BR 9807079A BR 9807079 A BR9807079 A BR 9807079A BR 9807079 A BR9807079 A BR 9807079A
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- alkyl
- hydroxy
- preparation
- pharmaceutical formulation
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0081—Substituted in position 17 alfa and 17 beta
- C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
- C07J1/0096—Alkynyl derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C07J21/006—Ketals at position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
- C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/001—Oxiranes
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Ophthalmology & Optometry (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Anesthesiology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
"COMPOSTO DE DERIVADO DE 16-HIDROXI-11-(FENIL SUBSTITUìDO)-ESTRA-4,9-DIENO, USO DE UM COMPOSTO, FORMULAçãO FARMACêUTICA, E, PROCESSO PARA A PREPARAçãO DE UM COMPOSTO". A presente invenção refere-se a derivados 16-hidróxi-11-(fenila substituída)-estra-4,9-dieno de acordo com a fórmula (I): em que R~ 1~ é alquila C~ 1-6, cicloalquila C~ 3-6~, alcóxi C~ 1-6~, triflato, piridila ou fenila, em que a porção fenila é opcionalmente substituída por um ou mais substituintes selecionados a partir de ciano, halogênio e alquila C~ 1-4~; R~ 2~ é hidrogênio, alquila C~ 1-6~-oxo-alquila C~ 1-6~, R~ 3~é hidrogênio, halogênio ou alquila C~ 1-6~, opcionalmente substituída por um aou mais substituintes selecionados a partir de alcóxi C~ 1-6~ e halogênio; R~ 4~ é hidrogênio, alquila C~ 1-6~, 1-oxo-alquila C~ 1-6~ ou carbóxi-1-oxo-alquila C~ 1-6~; e X é (H, OH), O ou NOH; ou um solvato ou sal farmaceuticamente aceitável dos mesmos; a processos para a sua preparação, a formulações farmacêuticas que os contenham e a seu uso em terapia médica, particularmente no tratamento ou profilaxia de sintomas ou doenças dependentes de glicocorticóide.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP97200098 | 1997-01-15 | ||
PCT/EP1998/000377 WO1998031702A1 (en) | 1997-01-15 | 1998-01-13 | 16-hydroxy-11-(substituted phenyl)-estra-4,9-diene derivatives |
Publications (1)
Publication Number | Publication Date |
---|---|
BR9807079A true BR9807079A (pt) | 2000-04-18 |
Family
ID=8227931
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR9807079-7A BR9807079A (pt) | 1997-01-15 | 1998-01-13 | Composto de derivado de 16-hidróxi-11- (fenil substituìdo) - estra-4,9-dieno, uso de um composto, formulação farmacêutica, e processo para a preparação de um composto. |
Country Status (22)
Country | Link |
---|---|
US (1) | US6072068A (pt) |
EP (1) | EP0973792B1 (pt) |
JP (1) | JP2001508079A (pt) |
KR (1) | KR20000070149A (pt) |
CN (1) | CN1248262A (pt) |
AR (1) | AR011409A1 (pt) |
AT (1) | ATE248854T1 (pt) |
AU (1) | AU736064B2 (pt) |
BR (1) | BR9807079A (pt) |
CA (1) | CA2277924A1 (pt) |
DE (1) | DE69817792T2 (pt) |
HU (1) | HUP0000901A3 (pt) |
ID (1) | ID22228A (pt) |
IL (1) | IL122740A (pt) |
NO (1) | NO313386B1 (pt) |
NZ (1) | NZ336790A (pt) |
PL (1) | PL334518A1 (pt) |
RU (1) | RU2187510C2 (pt) |
TR (1) | TR199902367T2 (pt) |
TW (1) | TW518339B (pt) |
WO (1) | WO1998031702A1 (pt) |
ZA (1) | ZA9884B (pt) |
Families Citing this family (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EA004886B1 (ru) * | 1999-04-30 | 2004-08-26 | Пфайзер Продактс Инк. | Модуляторы рецепторов глюкокортикоидов |
US6740645B1 (en) * | 1999-09-03 | 2004-05-25 | Research Triangle Institute | 17β-acyl-17α-propynyl-11β-(cyclic amino) aryl steroids and their derivatives having antagonist hormonal properties |
DE19961219A1 (de) * | 1999-12-15 | 2001-07-19 | Jenapharm Gmbh | 11beta-Phenylestratrien-Derivate mit Fluoralkylgruppen in der aromatischen Seitenkette, deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
US7713989B2 (en) | 2000-04-27 | 2010-05-11 | Dow Robert L | Glucocorticoid receptor modulators |
IL146057A (en) * | 2000-10-27 | 2007-09-20 | Pfizer Prod Inc | A process for the preparation of modulators of a non-steroidal glucocorticoid receptor |
ES2262612T3 (es) * | 2000-10-28 | 2006-12-01 | Pfizer Products Inc. | Moduladpres del receptor de glucocorticoides. |
EP1201660B1 (en) * | 2000-10-30 | 2005-08-31 | Pfizer Products Inc. | Glucocorticoid receptor modulators |
US7250408B2 (en) * | 2002-12-16 | 2007-07-31 | Bayer Schering Pharma Ag | Glucocorticoid receptor antagonists for prophylaxis and therapy of glucocorticoid-mediated hypogonadism, of sexual dysfunction and/or infertility |
UA94639C2 (ru) | 2007-02-02 | 2011-05-25 | Пфайзер Продактс Інк. | Трициклические соединения и их применение как модуляторов глюкокортикоидного рецептора |
BR112015000443A2 (pt) | 2012-07-10 | 2017-06-27 | Bayer Pharma AG | derivados de estra-1,3,5(10),16-tetraeno 3-substituídos, processo para a sua produção, preparações farmacêuticas que contêm os mesmos, bem como seu uso para a produção de medicamentos |
AP3826A (en) | 2013-02-21 | 2016-09-30 | Bayer Pharma Aktiengellschaft | Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (akr1 c3) |
CN113559075A (zh) | 2014-11-17 | 2021-10-29 | 康泰科思特生物制药公司 | 奥那司酮延长释放组合物和方法 |
BR112018005999A2 (pt) | 2015-09-25 | 2019-01-08 | Context Biopharma Inc | métodos para a produção de intermediários de onapristona |
AU2016370499B2 (en) | 2015-12-15 | 2022-06-30 | Context Biopharma Inc. | Amorphous onapristone compositions and methods of making the same |
JP6995757B2 (ja) * | 2015-12-23 | 2022-01-17 | オリック ファーマシューティカルズ,インク. | グルココルチコイド受容体の阻害剤 |
EP3394078A4 (en) * | 2015-12-23 | 2019-11-27 | Oric Pharmaceuticals, Inc. | GLUCOCORTICOID RECEPTOR INHIBITORS |
WO2017112904A1 (en) | 2015-12-23 | 2017-06-29 | Oric Pharmaceuticals, Inc. | Inhibitors of glucocorticoid receptor |
CN106397519A (zh) * | 2016-08-30 | 2017-02-15 | 天津市中升挑战生物科技有限公司 | 一种烯丙孕素的制备方法 |
SG11201903055UA (en) | 2016-10-07 | 2019-05-30 | Oric Pharmaceuticals Inc | Inhibitors of glucocorticoid receptor |
US20180148471A1 (en) | 2016-11-30 | 2018-05-31 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
AU2019414333A1 (en) * | 2018-12-28 | 2021-08-05 | Panda Consulting Llc | Short-acting selective glucocorticoid receptor modulators |
CN114456223B (zh) * | 2022-01-24 | 2023-07-21 | 湖南科益新生物医药有限公司 | 3-缩酮的合成方法 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2522328B1 (fr) * | 1982-03-01 | 1986-02-14 | Roussel Uclaf | Nouveaux produits derives de la structure 3-ceto 4,9 19-nor steroides, leur procede de preparation et leur application comme medicaments |
AU580843B2 (en) * | 1985-02-07 | 1989-02-02 | Schering Aktiengesellschaft | 11``-phenyl-gonanes, their manufacture and pharmaceutical preparations containing them |
-
1997
- 1997-12-24 IL IL12274097A patent/IL122740A/xx active IP Right Grant
-
1998
- 1998-01-06 ZA ZA9884A patent/ZA9884B/xx unknown
- 1998-01-12 TW TW087100392A patent/TW518339B/zh not_active IP Right Cessation
- 1998-01-13 ID IDW990700A patent/ID22228A/id unknown
- 1998-01-13 US US09/341,603 patent/US6072068A/en not_active Expired - Fee Related
- 1998-01-13 BR BR9807079-7A patent/BR9807079A/pt not_active IP Right Cessation
- 1998-01-13 WO PCT/EP1998/000377 patent/WO1998031702A1/en not_active Application Discontinuation
- 1998-01-13 JP JP53369598A patent/JP2001508079A/ja active Pending
- 1998-01-13 KR KR1019997006375A patent/KR20000070149A/ko not_active Application Discontinuation
- 1998-01-13 HU HU0000901A patent/HUP0000901A3/hu unknown
- 1998-01-13 RU RU99118008/04A patent/RU2187510C2/ru not_active IP Right Cessation
- 1998-01-13 CN CN98802618A patent/CN1248262A/zh active Pending
- 1998-01-13 DE DE69817792T patent/DE69817792T2/de not_active Expired - Fee Related
- 1998-01-13 TR TR1999/02367T patent/TR199902367T2/xx unknown
- 1998-01-13 PL PL98334518A patent/PL334518A1/xx unknown
- 1998-01-13 CA CA002277924A patent/CA2277924A1/en not_active Abandoned
- 1998-01-13 AT AT98906887T patent/ATE248854T1/de not_active IP Right Cessation
- 1998-01-13 NZ NZ336790A patent/NZ336790A/en unknown
- 1998-01-13 AU AU62935/98A patent/AU736064B2/en not_active Ceased
- 1998-01-13 EP EP98906887A patent/EP0973792B1/en not_active Expired - Lifetime
- 1998-01-14 AR ARP980100151A patent/AR011409A1/es not_active Application Discontinuation
-
1999
- 1999-07-14 NO NO19993459A patent/NO313386B1/no not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
ZA9884B (en) | 1998-07-08 |
JP2001508079A (ja) | 2001-06-19 |
NO313386B1 (no) | 2002-09-23 |
PL334518A1 (en) | 2000-02-28 |
ID22228A (id) | 1999-09-23 |
HUP0000901A3 (en) | 2001-07-30 |
CA2277924A1 (en) | 1998-07-23 |
RU2187510C2 (ru) | 2002-08-20 |
DE69817792T2 (de) | 2004-07-01 |
AU6293598A (en) | 1998-08-07 |
ATE248854T1 (de) | 2003-09-15 |
NO993459L (no) | 1999-09-07 |
DE69817792D1 (de) | 2003-10-09 |
KR20000070149A (ko) | 2000-11-25 |
TR199902367T2 (xx) | 2000-04-21 |
US6072068A (en) | 2000-06-06 |
AR011409A1 (es) | 2000-08-16 |
AU736064B2 (en) | 2001-07-26 |
WO1998031702A1 (en) | 1998-07-23 |
NO993459D0 (no) | 1999-07-14 |
TW518339B (en) | 2003-01-21 |
HUP0000901A2 (hu) | 2000-10-28 |
CN1248262A (zh) | 2000-03-22 |
EP0973792A1 (en) | 2000-01-26 |
NZ336790A (en) | 2000-06-23 |
IL122740A (en) | 2003-09-17 |
IL122740A0 (en) | 1998-08-16 |
EP0973792B1 (en) | 2003-09-03 |
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Legal Events
Date | Code | Title | Description |
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B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 7,8A E 9A 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 1888 DE 13/03/2007. |