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AR072533A1 - Derivados de estratrieno que comprenden bioisosteros heterociclicos para el anillo fenolico a - Google Patents

Derivados de estratrieno que comprenden bioisosteros heterociclicos para el anillo fenolico a

Info

Publication number
AR072533A1
AR072533A1 ARP090102822A ARP090102822A AR072533A1 AR 072533 A1 AR072533 A1 AR 072533A1 AR P090102822 A ARP090102822 A AR P090102822A AR P090102822 A ARP090102822 A AR P090102822A AR 072533 A1 AR072533 A1 AR 072533A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
optionally substituted
hydrogen
alkenyl
Prior art date
Application number
ARP090102822A
Other languages
English (en)
Inventor
Thorsten Blume
Dieter Heldmann
Norbert Schmees
Joachim Kuhnke
Tim Wintermantel
Christiane Otto
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 AR072533A1 publication Critical patent/AR072533A1/es

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)
  • Gynecology & Obstetrics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Hematology (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

Derivados de pirazolo-estrieno y triazolo-estrieno, composiciones farmacéuticas que los contienen y su uso en el tratamiento o la prevencion de trastornos y enfermedades mediados por un receptor de estrogeno, tales como los sofocos, la sequedad vaginal, la osteopenia, la osteoporosis, la hiperlipidemia, la pérdida de funcion cognitiva, las enfermedades degenerativas del cerebro, las enfermedades cardiovasculares, las enfermedades cerebrovasculares, los cánceres y la hiperplasia sensibles a hormonas (en tejidos que incluyen las mamas, el endometrio y el cuello uterino en las mujeres y la prostata en los hombres), la endometriosis, los fibroides uterinos, la osteoartritis; y como agentes anticonceptivos, solos o en combinacion con un progestogeno o un antagonista de un progestogeno. Los compuestos son moduladores selectivos dle receptor de estrogeno. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) donde X se selecciona entre el grupo que consiste de nitrogeno y CRa, donde Ra representa hidrogeno, grupo C1-3-alquilo, un grupo CpF2p+1 con p = 1-3, R2 representa un átomo de hidrogeno, un átomo de halogeno, un grupo C1-3-alquilo o un grupo trifluorometilo, R11 se selecciona entre el grupo de hidrogeno, halogeno, C1-3-alquilo, C2-3-alquenilo, C2-3-alquinilo y C1-3-alcoxi, R16 se selecciona entre el grupo que consiste de hidrogeno, hidroxilo, halogeno, C1-3-alquilo, C2-3-alquenilo, C2-3-alquinilo y trifluorometilo, R17a y R17b representan un átomo de hidrogeno, un grupo hidroxilo, un grupo C1-3-alquilo opcionalmente sustituido, un grupo C2-3-alquenilo opcionalmente sustituido, un grupo C2-3-alquinilo opcionalmente sustituido, donde dichos sustituyentes se seleccionan entre un grupo hidroxilo, fluor o un grupo OR donde R es un grupo C1-3-alquilo o R17a y R17b representan un átomo de halogeno, o un grupo -OCORb, donde Rb representa un grupo -(CH2)nCOOH con n = 2 or 3, o un grupo C1-5-alquilo con la condicion de que R17a representa un grupo hidroxilo, R17b representa un átomo de hidrogeno o un grupo C1-3-alquilo opcionalmente sustituido, un grupo C2-3-alquenilo opcionalmente sustituido o un grupo OCORb con la definicion de Rb como se definio precedentemente, y vice versa, o R17a y R17b representan juntos un átomo de oxígeno, y R18 representa un átomo de hidrogeno o un grupo metilo, o una sal aceptable farmacéuticamente del mismo.
ARP090102822A 2008-07-24 2009-07-24 Derivados de estratrieno que comprenden bioisosteros heterociclicos para el anillo fenolico a AR072533A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08161108A EP2147924A1 (en) 2008-07-24 2008-07-24 Estratriene derivatives comprising heterocyclic bioisosteres for the phenolic a-ring

Publications (1)

Publication Number Publication Date
AR072533A1 true AR072533A1 (es) 2010-09-01

Family

ID=40329347

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090102822A AR072533A1 (es) 2008-07-24 2009-07-24 Derivados de estratrieno que comprenden bioisosteros heterociclicos para el anillo fenolico a

Country Status (24)

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

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011092127A1 (en) * 2010-01-26 2011-08-04 Bayer Schering Pharma Aktiengesellschaft 14,17-bridged estratriene derivatives comprising heterocyclic bioisosteres for the phenolic a-ring
EP4151636A4 (en) * 2020-05-15 2024-02-28 Simcere Pharmaceutical Co. Ltd. PYRROLIDINE COMPOUND AND USE THEREOF
DE102022109556A1 (de) 2022-04-20 2023-10-26 Eberspächer Catem Gmbh & Co. Kg Elektrische Heizvorrichtung
DE102022109544A1 (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
WO2004005314A1 (en) * 2002-07-03 2004-01-15 Ortho-Mcneil Pharmaceutical, Inc. ESTRIENO[3,2-b]/[3,4-c]PYRROLE DERIVATIVES USEFUL AS MODULATORS OF THE ESTROGEN RECEPTORS

Also Published As

Publication number Publication date
ECSP11010780A (es) 2011-02-28
CL2011000153A1 (es) 2011-07-08
MA32477B1 (fr) 2011-07-03
AU2009273494A1 (en) 2010-01-28
CR20110045A (es) 2012-05-28
UY32005A (es) 2010-02-26
TW201008570A (en) 2010-03-01
CN102105484A (zh) 2011-06-22
CA2731634A1 (en) 2010-01-28
KR20110036739A (ko) 2011-04-08
BRPI0915987A2 (pt) 2019-09-24
EP2307439A1 (en) 2011-04-13
MX2011000939A (es) 2011-03-04
IL210314A0 (en) 2011-03-31
US20110190246A1 (en) 2011-08-04
SV2011003817A (es) 2011-05-20
JP2011528675A (ja) 2011-11-24
DOP2011000024A (es) 2011-02-28
EP2147924A1 (en) 2010-01-27
PE20110402A1 (es) 2011-06-19
WO2010009828A1 (en) 2010-01-28
EA201100226A1 (ru) 2011-08-30
CO6351799A2 (es) 2011-12-20
ZA201101445B (en) 2012-07-25

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