PE20110402A1 - Derivados de estratieno que comprende biososteros heterociclicos para el anillo fenolico a - Google Patents

Derivados de estratieno que comprende biososteros heterociclicos para el anillo fenolico a

Info

Publication number
PE20110402A1
PE20110402A1 PE2011000072A PE2011000072A PE20110402A1 PE 20110402 A1 PE20110402 A1 PE 20110402A1 PE 2011000072 A PE2011000072 A PE 2011000072A PE 2011000072 A PE2011000072 A PE 2011000072A PE 20110402 A1 PE20110402 A1 PE 20110402A1
Authority
PE
Peru
Prior art keywords
alkyl
pyrazolo
17beta
estra
trien
Prior art date
Application number
PE2011000072A
Other languages
English (en)
Inventor
Thorsten Blume
Dieter Heldmann
Norbert Schmees
Christiane Otto
Tim Wintermantel
Joachin 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 PE20110402A1 publication Critical patent/PE20110402A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0047—Nitrogen only at position 2(3)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • 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
    • 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

Abstract

SE REFIERE A UN COMPUESTO DERIVADO DE PIRAZOLO-ESTRIENO Y TRIAZOLO-ESTRIENO DE FORMULA (I) DONDE X ES N, CH, C(ALQUILO C1-C3), ENTRE OTROS; R2 ES H, HALOGENO, ALQUILO C1-C3 O GRUPO TRIFLUOROMETILO; R11 ES H, HALOGENO, ALQUILO C1-C3, ENTRE OTROS; R16 ES H, HIDROXILO, ALQUILO C1-C3, ENTRE OTROS; R17a Y R17b SON H, HIDROXILO, ALQUILO C1-C3, ENTRE OTROS; R18 ES H O METILO. SON COMPUESTOS PREFERIDOS 2'H-PIRAZOLO[3',4':3,4]ESTRA-1,3,5(10)-TRIEN-17BETA-OL; 17ALFA-METIL-2'-H-PIRAZOLO[3',4':3,4]ESTRA-1,3,5(10)-TRIEN-17BETA-OL; 17ALFA-ETIL-2'-H-PIRAZOLO[3',4':3,4]ESTRA-1,3,5(10)-TRIEN-17BETA-OL; ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICON FARMACEUTICA QUE ADMITE UN COMPUESTO ACTIVO ADICIONAL SELLECIONADO ENTRE UN MODULADOR SELECTIVO DEL RECEPTOR DE ESTROGENO (SERM), UN DESESTABILIZADOR SELECTIVO DEL RECEPTOR DE ESTROGENO ( SERD) O UN PROGESTAGENO. DICHO COMPUESTO ES UN AGONISTA DEL RECEPTOR DE ESTROGENO UTIL EN LA ANTICONCEPCION Y EL TRATAMIENTO DE SOFOCOS, SEQUEDAD VAGINAL, OSTEOPENIA, OSTEOPOROSIS, HIPERLIPIDEMIA, ENTRE OTROS
PE2011000072A 2008-07-24 2009-07-14 Derivados de estratieno que comprende biososteros heterociclicos para el anillo fenolico a PE20110402A1 (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
PE20110402A1 true PE20110402A1 (es) 2011-06-19

Family

ID=40329347

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011000072A PE20110402A1 (es) 2008-07-24 2009-07-14 Derivados de estratieno que comprende biososteros 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
CN115836068A (zh) * 2020-05-15 2023-03-21 先声药业有限公司 吡咯烷类化合物及其应用
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
ATE376555T1 (de) * 2002-07-03 2007-11-15 Ortho Mcneil Pharm Inc Estrieno(3,2-b)/(3,4-c)pyrrole derivative als modulatoren des östrogen rezeptors

Also Published As

Publication number Publication date
EP2147924A1 (en) 2010-01-27
ECSP11010780A (es) 2011-02-28
AU2009273494A1 (en) 2010-01-28
DOP2011000024A (es) 2011-02-28
IL210314A0 (en) 2011-03-31
SV2011003817A (es) 2011-05-20
WO2010009828A1 (en) 2010-01-28
MA32477B1 (fr) 2011-07-03
ZA201101445B (en) 2012-07-25
AR072533A1 (es) 2010-09-01
UY32005A (es) 2010-02-26
MX2011000939A (es) 2011-03-04
CA2731634A1 (en) 2010-01-28
EP2307439A1 (en) 2011-04-13
BRPI0915987A2 (pt) 2019-09-24
JP2011528675A (ja) 2011-11-24
EA201100226A1 (ru) 2011-08-30
CL2011000153A1 (es) 2011-07-08
CO6351799A2 (es) 2011-12-20
TW201008570A (en) 2010-03-01
KR20110036739A (ko) 2011-04-08
CN102105484A (zh) 2011-06-22
US20110190246A1 (en) 2011-08-04
CR20110045A (es) 2012-05-28

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