MA32477B1 - Derives estratrienes comprenant des bioisosteres heterocycliques pour le cycle a phenolique - Google Patents

Derives estratrienes comprenant des bioisosteres heterocycliques pour le cycle a phenolique

Info

Publication number
MA32477B1
MA32477B1 MA33521A MA33521A MA32477B1 MA 32477 B1 MA32477 B1 MA 32477B1 MA 33521 A MA33521 A MA 33521A MA 33521 A MA33521 A MA 33521A MA 32477 B1 MA32477 B1 MA 32477B1
Authority
MA
Morocco
Prior art keywords
stratrini
bioesostere
heterozygous
phenolic
estriene
Prior art date
Application number
MA33521A
Other languages
Arabic (ar)
English (en)
Inventor
Thorsten Blume
Dieter Heldmann
Norbert Schmees
Christiane Otto
Tim Wintermantel
Joachim Kuhnke
Original Assignee
Bayer Schering Pharma Ag
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 Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of MA32477B1 publication Critical patent/MA32477B1/fr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036Nitrogen-containing hetero ring
    • C07J71/0042Nitrogen only
    • C07J71/0047Nitrogen only at position 2(3)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)

Abstract

La présente invention concerne de nouveaux dérivés pyrazolo-estriènes et triazolo-estriènes, des compositions pharmaceutiques les contenant et leur utilisation dans le traitement ou la prévention de troubles et de maladies médiés par un récepteur d'sstrogène tels que les bouffées de chaleur, la sécheresse vaginale, l'ostéopénie, l'ostéoporose, l'hyperlipidémie, la perte de la fonction cognitive, les maladies cérébrales dégénératives, les maladies cardiovasculaires, les maladies cérébrovasculaires, les cancers hormono-sensibles et l'hyperplasie (dans les tissus comprenant le sein, l'endomètre, et le col de l'utérus chez les femmes, et la prostate chez les hommes), l'endométriosse, les fibroïdes utérins, l'arthrose ; et comme agents contraceptifs soit seuls soit en association avec un progestogène ou un antagoniste de progestogène. Les composés de l'invention sont des modulateurs sélectifs des récepteurs d'oestrogène.
MA33521A 2008-07-24 2011-01-14 Derives estratrienes comprenant des bioisosteres heterocycliques pour le cycle a phenolique MA32477B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08161108A EP2147924A1 (fr) 2008-07-24 2008-07-24 Dérivés d'estratriènes comportant des bioisostères pour l'anneau phénolique
PCT/EP2009/005086 WO2010009828A1 (fr) 2008-07-24 2009-07-14 Dérivés estratriènes comprenant des dioisostères hétérocycliques pour le cycle a phénolique

Publications (1)

Publication Number Publication Date
MA32477B1 true MA32477B1 (fr) 2011-07-03

Family

ID=40329347

Family Applications (1)

Application Number Title Priority Date Filing Date
MA33521A MA32477B1 (fr) 2008-07-24 2011-01-14 Derives estratrienes comprenant des bioisosteres heterocycliques pour le cycle a phenolique

Country Status (24)

Country Link
US (1) US20110190246A1 (fr)
EP (2) EP2147924A1 (fr)
JP (1) JP2011528675A (fr)
KR (1) KR20110036739A (fr)
CN (1) CN102105484A (fr)
AR (1) AR072533A1 (fr)
AU (1) AU2009273494A1 (fr)
BR (1) BRPI0915987A2 (fr)
CA (1) CA2731634A1 (fr)
CL (1) CL2011000153A1 (fr)
CO (1) CO6351799A2 (fr)
CR (1) CR20110045A (fr)
DO (1) DOP2011000024A (fr)
EA (1) EA201100226A1 (fr)
EC (1) ECSP11010780A (fr)
IL (1) IL210314A0 (fr)
MA (1) MA32477B1 (fr)
MX (1) MX2011000939A (fr)
PE (1) PE20110402A1 (fr)
SV (1) SV2011003817A (fr)
TW (1) TW201008570A (fr)
UY (1) UY32005A (fr)
WO (1) WO2010009828A1 (fr)
ZA (1) ZA201101445B (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011092127A1 (fr) * 2010-01-26 2011-08-04 Bayer Schering Pharma Aktiengesellschaft Dérivés d'estratriène 14,17-pontés comprenant des bioisostères hétérocycliques pour le noyau phénolique a
JP2023526568A (ja) * 2020-05-15 2023-06-21 シムサー ファーマシューティカル カンパニー リミテッド ピロリジン化合物及びその使用
DE102022109544A1 (de) 2022-04-20 2023-10-26 Eberspächer Catem Gmbh & Co. Kg Elektrische Heizvorrichtung
DE102022109556A1 (de) 2022-04-20 2023-10-26 Eberspächer Catem Gmbh & Co. Kg Elektrische Heizvorrichtung

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3458504A (en) * 1966-10-24 1969-07-29 Sterling Drug Inc Steroido(3,4-c)pyrazoles of the 5alpha- and 5beta-androstane series
DE60317109T2 (de) * 2002-07-03 2008-07-31 Ortho-Mcneil Pharmaceutical, Inc. Estrienoä3,2-bü/ä3,4-cüpyrrole derivative als modulatoren des östrogen rezeptors

Also Published As

Publication number Publication date
KR20110036739A (ko) 2011-04-08
JP2011528675A (ja) 2011-11-24
EA201100226A1 (ru) 2011-08-30
WO2010009828A1 (fr) 2010-01-28
CA2731634A1 (fr) 2010-01-28
ECSP11010780A (es) 2011-02-28
BRPI0915987A2 (pt) 2019-09-24
CN102105484A (zh) 2011-06-22
AR072533A1 (es) 2010-09-01
CR20110045A (es) 2012-05-28
UY32005A (es) 2010-02-26
CO6351799A2 (es) 2011-12-20
MX2011000939A (es) 2011-03-04
ZA201101445B (en) 2012-07-25
AU2009273494A1 (en) 2010-01-28
EP2307439A1 (fr) 2011-04-13
CL2011000153A1 (es) 2011-07-08
DOP2011000024A (es) 2011-02-28
EP2147924A1 (fr) 2010-01-27
PE20110402A1 (es) 2011-06-19
TW201008570A (en) 2010-03-01
SV2011003817A (es) 2011-05-20
IL210314A0 (en) 2011-03-31
US20110190246A1 (en) 2011-08-04

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