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.

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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
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BR
Brazil
Prior art keywords
compound
alkyl
hydroxy
preparation
pharmaceutical formulation
Prior art date
Application number
BR9807079-7A
Other languages
English (en)
Inventor
Marinus Bernard Groen
Ronald Gebhard
Original Assignee
Akzo Nobel 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 Akzo Nobel Nv filed Critical Akzo Nobel Nv
Publication of BR9807079A publication Critical patent/BR9807079A/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0081Substituted in position 17 alfa and 17 beta
    • C07J1/0088Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
    • C07J1/0096Alkynyl derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005Ketals
    • C07J21/006Ketals at position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077Normal 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
    • C07J41/0083Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (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.
BR9807079-7A 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. BR9807079A (pt)

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)

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MXPA01011018A (es) 1999-04-30 2002-05-06 Pfizer Prod Inc Moduladores del receptor glucocorticoide.
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
PT2114970E (pt) 2007-02-02 2011-09-22 Pfizer Prod Inc Compostos tricíclicos e sua utilização como moduladores de receptor de glucocorticóide
ES2603258T3 (es) 2012-07-10 2017-02-24 Bayer Pharma Aktiengesellschaft Derivados de estra-1,3,5(10),16-tetraeno 3-sustituidos, procedimiento para su preparación, preparaciones farmacéuticas que los contienen así como su uso para la preparación de medicamentos
MA38349A1 (fr) 2013-02-21 2017-02-28 Bayer Pharma AG Œstra-1,3,5(10),16-tétraéno-3-carboxamide pour inhiber la 17-bêta-hydroxystéroïde déshydrogénase (akr1c3)
KR20170084086A (ko) 2014-11-17 2017-07-19 아르노 테라퓨틱스 인코포레이티드 오나프리스톤 연장-방출 조성물 및 방법
CA2998924A1 (en) 2015-09-25 2017-03-30 Context Biopharma Inc. Methods of making onapristone intermediates
US10548905B2 (en) 2015-12-15 2020-02-04 Context Biopharma Inc. Amorphous onapristone compositions and methods of making the same
AU2016377702B2 (en) * 2015-12-23 2021-03-11 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
WO2017112904A1 (en) 2015-12-23 2017-06-29 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
US11208432B2 (en) 2015-12-23 2021-12-28 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
CN111690031B (zh) 2016-10-07 2021-06-01 欧瑞克制药公司 糖皮质激素受体抑制剂
US20180148471A1 (en) 2016-11-30 2018-05-31 Arno Therapeutics, Inc. Methods for onapristone synthesis dehydration and deprotection
JP2022515528A (ja) * 2018-12-28 2022-02-18 パンダ コンサルティング エルエルシー 短時間作用型選択的糖質コルチコイド受容体モジュレーター
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

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* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
CN1248262A (zh) 2000-03-22
AU736064B2 (en) 2001-07-26
NO993459L (no) 1999-09-07
EP0973792B1 (en) 2003-09-03
DE69817792D1 (de) 2003-10-09
WO1998031702A1 (en) 1998-07-23
RU2187510C2 (ru) 2002-08-20
EP0973792A1 (en) 2000-01-26
TR199902367T2 (xx) 2000-04-21
US6072068A (en) 2000-06-06
DE69817792T2 (de) 2004-07-01
JP2001508079A (ja) 2001-06-19
AR011409A1 (es) 2000-08-16
AU6293598A (en) 1998-08-07
ID22228A (id) 1999-09-23
IL122740A (en) 2003-09-17
KR20000070149A (ko) 2000-11-25
NO993459D0 (no) 1999-07-14
TW518339B (en) 2003-01-21
HUP0000901A2 (hu) 2000-10-28
NZ336790A (en) 2000-06-23
PL334518A1 (en) 2000-02-28
ZA9884B (en) 1998-07-08
HUP0000901A3 (en) 2001-07-30
IL122740A0 (en) 1998-08-16
ATE248854T1 (de) 2003-09-15
CA2277924A1 (en) 1998-07-23
NO313386B1 (no) 2002-09-23

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