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AR011409A1 - Derivados de 16-hidroxi-11-(fenil substituido)-estra-4,9-dieno, su utilizacion, un procedimiento para prepararlos, formulaciones farmaceuticasque comprenden a dichos derivados, y un compuesto utilizable como intermediario para prepararlos - Google Patents

Derivados de 16-hidroxi-11-(fenil substituido)-estra-4,9-dieno, su utilizacion, un procedimiento para prepararlos, formulaciones farmaceuticasque comprenden a dichos derivados, y un compuesto utilizable como intermediario para prepararlos

Info

Publication number
AR011409A1
AR011409A1 ARP980100151A ARP980100151A AR011409A1 AR 011409 A1 AR011409 A1 AR 011409A1 AR P980100151 A ARP980100151 A AR P980100151A AR P980100151 A ARP980100151 A AR P980100151A AR 011409 A1 AR011409 A1 AR 011409A1
Authority
AR
Argentina
Prior art keywords
derivatives
prepare
6alkyl
oxo
estra
Prior art date
Application number
ARP980100151A
Other languages
English (en)
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 AR011409A1 publication Critical patent/AR011409A1/es

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

Abstract

Derivados de 16-hidroxi-11-(fenilo substituido)-estra-4,9-dieno de acuerdo con la formula (I), donde R1 es C1-6 alquil, C3-6 cicloalquil, C1-6alcoxi, triflato, piridil o fenilo donde la parte de fenilo opcionalmente se substituye por unoo más substituyentes seleccionados entre ciano, halogeno yC1-4alquil; R2 es hidrogeno, C1-6alquil, 1-oxo-C1-6 alquil o carboxi-1-oxo- C1-6 alquil; R3 es hidrogeno, halogeno o C1-6 alquil opcionalmente substituidopor uno o más substituyentesselec cionados entre C1-6 alcoxi y halogeno; R4 es hidrogeno, C1-6 alquil, 1-oxo-C1-6 alquil o carboxi-1-oxo-C1-6 alquil; yX es (H, OH), O o NOH; o una sal o solvato farmacéuticamente aceptable del mismo; un procedimiento de preparacion,formulacione s farmacéuticas que loscontienen y su uso en terapia médica, en particular en el tratamiento o profilaxis de enfermedades o síntomas glucocorticoide dependientes; y uncompuesto utilizable como intermediario para preparar a estosderivados.
ARP980100151A 1997-01-15 1998-01-14 Derivados de 16-hidroxi-11-(fenil substituido)-estra-4,9-dieno, su utilizacion, un procedimiento para prepararlos, formulaciones farmaceuticasque comprenden a dichos derivados, y un compuesto utilizable como intermediario para prepararlos AR011409A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP97200098 1997-01-15

Publications (1)

Publication Number Publication Date
AR011409A1 true AR011409A1 (es) 2000-08-16

Family

ID=8227931

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980100151A AR011409A1 (es) 1997-01-15 1998-01-14 Derivados de 16-hidroxi-11-(fenil substituido)-estra-4,9-dieno, su utilizacion, un procedimiento para prepararlos, formulaciones farmaceuticasque comprenden a dichos derivados, y un compuesto utilizable como intermediario para prepararlos

Country Status (22)

Country Link
US (1) US6072068A (es)
EP (1) EP0973792B1 (es)
JP (1) JP2001508079A (es)
KR (1) KR20000070149A (es)
CN (1) CN1248262A (es)
AR (1) AR011409A1 (es)
AT (1) ATE248854T1 (es)
AU (1) AU736064B2 (es)
BR (1) BR9807079A (es)
CA (1) CA2277924A1 (es)
DE (1) DE69817792T2 (es)
HU (1) HUP0000901A3 (es)
ID (1) ID22228A (es)
IL (1) IL122740A (es)
NO (1) NO313386B1 (es)
NZ (1) NZ336790A (es)
PL (1) PL334518A1 (es)
RU (1) RU2187510C2 (es)
TR (1) TR199902367T2 (es)
TW (1) TW518339B (es)
WO (1) WO1998031702A1 (es)
ZA (1) ZA9884B (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ514465A (en) * 1999-04-30 2003-11-28 Pfizer Prod Inc Glucocorticoid receptor modulators
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
JP2002193911A (ja) * 2000-10-28 2002-07-10 Pfizer Prod Inc グルココルチコイドレセプターモジュレーター
ES2246292T3 (es) 2000-10-30 2006-02-16 Pfizer Products Inc. Moduladores de receptor glucocorticoide.
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
KR101107949B1 (ko) 2007-02-02 2012-02-08 화이자 프로덕츠 인코포레이티드 트라이사이클릭 화합물 및 글루코코르티코이드 수용체 조절자로서의 이들의 용도
RU2326673C1 (ru) * 2007-02-27 2008-06-20 ФГУ Национальный научный центр наркологии Росздрава ПРИМЕНЕНИЕ 17α-АЦЕТАТ-21-ПИВАЛОАТ 17α,21-ДИГИДРОКСИПРЕГН-4-ЕН-3,20-ДИОНА В КАЧЕСТВЕ СРЕДСТВА, СНИЖАЮЩЕГО ПАТОЛОГИЧЕСКОЕ ВЛЕЧЕНИЕ К КОКАИНУ
JP6196302B2 (ja) 2012-07-10 2017-09-13 バイエル・ファルマ・アクティエンゲゼルシャフト 3−置換エストラ−1,3,5(10),16−テトラエン誘導体、その調製法、これらを含む医薬製剤および医薬を調製するためのその使用
SG11201505875WA (en) 2013-02-21 2015-09-29 Bayer Pharma AG 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
KR20180113988A (ko) 2015-12-15 2018-10-17 컨텍스트 바이오파마 인코포레이티드 비정질 오나프리스톤 조성물 및 그 제조방법
EP3394079A4 (en) * 2015-12-23 2019-08-21 Oric Pharmaceuticals, Inc. INHIBITORS OF GLUCOCORTICOIDREZEPTORS
US11110103B2 (en) 2015-12-23 2021-09-07 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
EP3394078A4 (en) * 2015-12-23 2019-11-27 Oric Pharmaceuticals, Inc. INHIBITORS OF THE GLUCOCORTICIDE 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
DK3523315T3 (da) * 2016-10-07 2021-05-03 Oric Pharmaceuticals Inc Inhibitor af glucocorticoidreceptor
US20180148471A1 (en) 2016-11-30 2018-05-31 Arno Therapeutics, Inc. Methods for onapristone synthesis dehydration and deprotection
CA3125151A1 (en) * 2018-12-28 2020-07-02 Panda Consulting Llc Short-acting selective glucocorticoid receptor modulators
WO2023000135A1 (en) * 2021-07-19 2023-01-26 Context Biopharma Inc. Processes of making onapristone and intermediates thereof
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)

* 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
NZ214998A (en) * 1985-02-07 1989-06-28 Schering Ag 13-(methyl or ethyl)-11-beta-phenyl-gonane derivatives; preparatory processes and pharmaceutical compositions

Also Published As

Publication number Publication date
HUP0000901A3 (en) 2001-07-30
DE69817792T2 (de) 2004-07-01
NO993459D0 (no) 1999-07-14
TW518339B (en) 2003-01-21
NO313386B1 (no) 2002-09-23
RU2187510C2 (ru) 2002-08-20
HUP0000901A2 (hu) 2000-10-28
NO993459L (no) 1999-09-07
EP0973792A1 (en) 2000-01-26
ATE248854T1 (de) 2003-09-15
IL122740A0 (en) 1998-08-16
ID22228A (id) 1999-09-23
KR20000070149A (ko) 2000-11-25
WO1998031702A1 (en) 1998-07-23
ZA9884B (en) 1998-07-08
AU736064B2 (en) 2001-07-26
TR199902367T2 (xx) 2000-04-21
US6072068A (en) 2000-06-06
NZ336790A (en) 2000-06-23
IL122740A (en) 2003-09-17
AU6293598A (en) 1998-08-07
EP0973792B1 (en) 2003-09-03
BR9807079A (pt) 2000-04-18
PL334518A1 (en) 2000-02-28
JP2001508079A (ja) 2001-06-19
CN1248262A (zh) 2000-03-22
CA2277924A1 (en) 1998-07-23
DE69817792D1 (de) 2003-10-09

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