[go: up one dir, main page]

PE20060314A1 - ESTRIOL AND STETROL PRODROGS - Google Patents

ESTRIOL AND STETROL PRODROGS

Info

Publication number
PE20060314A1
PE20060314A1 PE2005000555A PE2005000555A PE20060314A1 PE 20060314 A1 PE20060314 A1 PE 20060314A1 PE 2005000555 A PE2005000555 A PE 2005000555A PE 2005000555 A PE2005000555 A PE 2005000555A PE 20060314 A1 PE20060314 A1 PE 20060314A1
Authority
PE
Peru
Prior art keywords
sulfamoylbenzoate
ilo
trien
steroid
prodrogs
Prior art date
Application number
PE2005000555A
Other languages
Spanish (es)
Inventor
Peter Droescher
Walter Elger
Alexander Hillisch
Gudrun Reddersen
Ralf Wyrwa
Sven Ring
Birgitt Schneider
Original Assignee
Schering 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34969311&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20060314(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Ag filed Critical Schering Ag
Publication of PE20060314A1 publication Critical patent/PE20060314A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
    • 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
    • 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
    • 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
    • A61P5/26—Androgens
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/34—Gestagens

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A PRODROGAS DE ESTRIOL Y ESTEROL DE FORMULA (I), EN DONDE EL GRUPO Y ESTA UNIDO AL ESTEROIDE QUE DEBE SER LIBERADO, DONDE n ES DE 0 A 4; Y CUANDO R1, R2 O R3 ES INDEPENDIENTEMENTE -SO2NH2 O -NHSO2NH2, EL RESTO DE SUSTITUYENTES TOMAN EL VALOR DE H, FLUOR, Cl, OH O METOXI; R4, R16 Y R17, SON INDEPENDIENTEMENTE OH, TRIMETILSILILOXI, TER-BUTILDIMETILSILILOXI, BENZOATO, ENTRE OTROS; R15 ES PREFERENTEMENTE H; ESTEROIDE ES UN SISTEMA DE ANILLO ABCD DE FORULAS DE IIA A IID. SON COMPUESTOS PREFERIDOS: 3'-SULFAMOILBENZOATO DE 3,16*-DIHIDROXIESTRA-1,3,5(10)-TRIEN-17ß-ILO, 3'-SULFAMOILBENZOATO DE 3,17ß-DIHIDROXIESTRA-1,3,5(10)-TRIEN-16*-ILO, 4'-SULFAMOILBENZOATO DE 3,15*,17ß-TRIHIDROXIESTRA-1,3,5(10)-TRIEN-17ß-ILO, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMEINTO DE ELABORACION Y UNA COMPOSICION FARMACEUTICA QUE ADEMAS CONTIENE POR LO MENOS OTRO ESTEROIDE TAL COMO UN GESTAGENO COMO PROGESTERONA, NORETISTERONA, DIENOGEST, ENTRE OTROS. SIENDO UTIL PARA TERAPIA DE REEMPLAZO HORMONAL, TRATAMIENTO DE ENDOMETRIOSIS, CARCINOMA DE MAMA O PROSTATA, HIPOGONADISMOREFERS TO PRODROGS OF ESTRIOL AND STEROL OF FORMULA (I), WHERE THE GROUP AND IS JOINED TO THE STEROID THAT MUST BE RELEASED, WHERE n IS FROM 0 TO 4; AND WHEN R1, R2 OR R3 IS INDEPENDENTLY -SO2NH2 OR -NHSO2NH2, THE REST OF THE SUBSTITUENTS TAKE THE VALUE OF H, FLUOR, Cl, OH OR METOXY; R4, R16 AND R17 ARE INDEPENDENTLY OH, TRIMETHYLSILILOXY, TER-BUTYLDIMETHYLSILYLOXY, BENZOATE, AMONG OTHERS; R15 IS PREFERREDLY H; STEROID IS AN ABCD RING SYSTEM OF FORULAS FROM IIA TO IID. THE PREFERRED COMPOUNDS ARE: 3,16 * -DIHYDROXYSTRA-1,3,5 (10) -TRIEN-17ß-ILO 3'-SULFAMOYLBENZOATE, 3,17ß-DIHYDROXYSTRA-1,3,5 (10) -SULFAMOYLBENZOATE -TRIEN-16 * -ILO, 3,15 *, 17ß-TRIHYDROXYSTRA-1,3,5 (10) -TRIEN-17ß-ILO 4'-SULFAMOYLBENZOATE, AMONG OTHERS. IT ALSO REFERS TO A PREPARATION PROCEDURE AND A PHARMACEUTICAL COMPOSITION THAT ALSO CONTAINS AT LEAST ANOTHER STEROID SUCH AS A GESTAGEN LIKE PROGESTERONE, NORETISTERONE, DIENOGEST, AMONG OTHERS. BEING USEFUL FOR HORMONE REPLACEMENT THERAPY, TREATMENT OF ENDOMETRIOSIS, CARCINOMA OF THE BREAST OR PROSTATE, HYPOGONADISM

PE2005000555A 2004-05-21 2005-05-20 ESTRIOL AND STETROL PRODROGS PE20060314A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004025985A DE102004025985A1 (en) 2004-05-21 2004-05-21 Estriol and estetrol prodrugs

Publications (1)

Publication Number Publication Date
PE20060314A1 true PE20060314A1 (en) 2006-05-25

Family

ID=34969311

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005000555A PE20060314A1 (en) 2004-05-21 2005-05-20 ESTRIOL AND STETROL PRODROGS

Country Status (11)

Country Link
EP (1) EP1747231A1 (en)
JP (1) JP2007538027A (en)
AR (1) AR049108A1 (en)
DE (1) DE102004025985A1 (en)
GT (1) GT200500120A (en)
PA (1) PA8633801A1 (en)
PE (1) PE20060314A1 (en)
SV (1) SV2006002122A (en)
TW (1) TW200612962A (en)
UY (1) UY28910A1 (en)
WO (1) WO2005113576A1 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10027887A1 (en) 2000-05-31 2001-12-13 Jenapharm Gmbh Compounds with a sulfonamide group and pharmaceutical compositions containing these compounds
DE102004025966A1 (en) * 2004-05-21 2005-12-15 Schering Ag Estradiol prodrugs
US7534780B2 (en) 2004-05-21 2009-05-19 Bayer Schering Pharma Aktiengesellschaft Estradiol prodrugs
DE102005057224A1 (en) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag New 9-alpha substituted estratriene derivatives esterified with a sulfamoylphenyl-substituted acid residue, are prodrugs useful as carboanhydrase inhibitors for treating estrogen deficiency disorders
DE102005057408A1 (en) * 2005-11-30 2007-05-31 Bayer Schering Pharma Ag New sulfamoylsulfonate prodrugs e.g. useful for protecting red blood cells from attack by parasites or for hormone replacement therapy, female fertility control or treating hormone-associated diseases
CN100396693C (en) * 2006-11-08 2008-06-25 浙江大学 Preparation method of 1,4-pregnane-16β-methyl-17α,21-dihydroxy
CN102079771B (en) * 2010-12-10 2012-10-03 郑州大学 Estrogen amino-acid ester compound with antitumor activity as well as synthetic method thereof

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1238739A (en) * 1958-08-04 1960-08-19 Chimiotherapie Lab Franc Process for the preparation of water-soluble testosterone derivatives
FR8290M (en) * 1968-12-31 1970-11-09 Rech Chimiques Et Ind Mar Lab
US5001234A (en) * 1987-04-16 1991-03-19 The Upjohn Company Cyclic hydrocarbons with an aminoalkyl sidechain
US5116828A (en) * 1989-10-26 1992-05-26 Nippon Zoki Pharmaceutical Co., Ltd. Pharmaceutical composition for treatment of osteoporosis
US5571933A (en) * 1994-11-17 1996-11-05 Duquesne University Of The Holy Ghost Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use
DE19712488A1 (en) * 1997-03-25 1998-10-01 Knoell Hans Forschung Ev Steroid sulfamates, processes for their preparation and use thereof
EP1284272A4 (en) * 2000-04-24 2003-09-10 Kyowa Hakko Kogyo Kk Estra-1,3,5(10)-triene derivatives
DE10027887A1 (en) * 2000-05-31 2001-12-13 Jenapharm Gmbh Compounds with a sulfonamide group and pharmaceutical compositions containing these compounds
GB0015876D0 (en) * 2000-06-28 2000-08-23 Novartis Ag Organic compounds
GB0316290D0 (en) * 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
TWI331154B (en) * 2003-11-12 2010-10-01 Solvay Pharm Gmbh Novel 17-hydroxysteroid dehydrogenase type i inhibitors
DE102004025966A1 (en) * 2004-05-21 2005-12-15 Schering Ag Estradiol prodrugs

Also Published As

Publication number Publication date
PA8633801A1 (en) 2006-03-24
SV2006002122A (en) 2006-05-09
EP1747231A1 (en) 2007-01-31
AR049108A1 (en) 2006-06-28
TW200612962A (en) 2006-05-01
UY28910A1 (en) 2005-12-30
GT200500120A (en) 2006-01-24
DE102004025985A1 (en) 2005-12-15
WO2005113576A1 (en) 2005-12-01
JP2007538027A (en) 2007-12-27

Similar Documents

Publication Publication Date Title
RU2221569C2 (en) ANDROST-5-ENE-3β,17β-DIOL-CONTAINING PHARMACEUTICAL COMPOSITIONS AND ITS USING
PH30747A (en) Combination therapy for the treatment of estrogen sensitive disease.
BRPI0516243C1 (en) use of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3b,17b-diol and 4-androsten-3,17-dione, use of said precursor in association with a selective estrogen receptor modulator for uterine and mammary gland protection against cancer, pharmaceutical composition and kit
TW200716137A (en) Tanaproget compositions containing ethinyl estradiol
DE69434697D1 (en) Therapeutic uses of dehydroepiandrosterone for the treatment of decreased libido and osteoporosis
WO2001068074A3 (en) Pharmaceutical compositions of conjugated estrogens and methods of analyzing mixtures containing estrogenic compounds
BR0114801A (en) Tissue selective androgen receptor modulator compound, composition, pharmaceutical composition, method for binding a selective androgen receptor modulator compound to an androgen receptor, method for modulating spermatogenesis in an individual, method of hormone therapy, method for the treatment for an individual having a hormone-related condition, method for treating an individual having prostate cancer, and method for determining the presence of a compound
WO1999063974A3 (en) Selective estrogen receptor modulator in combination with denydroepiandrosterone (dhea) or analogues
RU2001101492A (en) PHARMACEUTICAL COMPOSITIONS CONTAINING ANDROST-5-EH-3-β, 17β-DIOL, AND ITS USE
NO20090578L (en) Pharmaceutical composition containing a tetrahydrofolic acid
CR8800A (en) PROGESTERONE RECEIVER ANTI-CONCEPTS AND ANTI-CONCEPTIVE SYSTEMS
JP4716726B2 (en) New etonogestrel ester
ATE452641T1 (en) ORAL PHARMACEUTICAL COMPOSITION CONTAINING 15-HYDROXYTESTOSTERONE AND ITS DERIVATIVES
CA2431645A1 (en) Methods of treating hormonal deficiencies in women undergoing estrogen replacement therapy
PE20060314A1 (en) ESTRIOL AND STETROL PRODROGS
WO2004006936A8 (en) Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy
RU2009102772A (en) 18-METHYL-19-NORANDROST-4-EN-17, 17-SPIROESTER (18-METHYL-19-NOR-20-SPIROX-4-EN-3-OH) AND PHARMACEUTICALS THAT CONTAIN
WO2005077968A3 (en) 17-methylene-or 17 - spiro - cyclopropane 7 - substituted estra - 1, 3, 5 (10) - triene derivatives with anti - estrogenic activity
RU2001101892A (en) TESTOSTERONE DERIVATIVE
MXPA05010871A (en) Methods of administering estrogens and progestins.
EA200601089A1 (en) TRANSDERMAL DELIVERY OF HORMONES WITHOUT THE NEED TO USE AGENTS, STRENGTHENING PENETRATION
EA200501739A1 (en) COMPOSITION CONTAINING PROTESTERONE RECEPTOR ANTAGONISTS AND PURE ANTIESTROGENS INTRODUCED FOR THE PREVENTION AND TREATMENT OF HORMONIZED DISEASES
BR0108411A (en) Male contraceptive formulation comprising norethisterone
KR970701538A (en) DESOGESTREL-CONTAINING TRANSDERMAL VAPPLICATION AGENT
BR0112791A (en) 16alpha-substituted steroidal compound, use thereof, treatment methods for selective activation of alpha subtype estrogen receptors, and for hormone replacement therapy or contraception, and, pharmaceutical composition

Legal Events

Date Code Title Description
FC Refusal