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PE20040157A1 - Progestinas no esteroides - Google Patents

Progestinas no esteroides

Info

Publication number
PE20040157A1
PE20040157A1 PE2003000244A PE2003000244A PE20040157A1 PE 20040157 A1 PE20040157 A1 PE 20040157A1 PE 2003000244 A PE2003000244 A PE 2003000244A PE 2003000244 A PE2003000244 A PE 2003000244A PE 20040157 A1 PE20040157 A1 PE 20040157A1
Authority
PE
Peru
Prior art keywords
compound
trifluoromethylphenyl
cyclopropyl
hydroxy
derivative
Prior art date
Application number
PE2003000244A
Other languages
English (en)
Inventor
Christa Hegele-Hartung
Manfred Lehmann
Norbert Schmees
Peter Muhn
Ulrike Fuhrmann
Michael Klotzbucher
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
Priority claimed from EP02005530A external-priority patent/EP1344776A1/en
Application filed by Schering Ag filed Critical Schering Ag
Publication of PE20040157A1 publication Critical patent/PE20040157A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P15/18Feminine contraceptives
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/021,2-Oxazines; Hydrogenated 1,2-oxazines

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 Y R2 SON -H O -F; R3 ES -CH3 O -CF3; AR ES EL GRUPO (a) Y EL GRUPO (b) O UN DERIVADO O ANALOGO DEL MISMO ACEPTABLE PARA USO FARMACEUTICO CON LA CONDICION QUE NO SEA 5-[3-{1-(3-TRIFLUOROMETILFENIL)-CICLOPROPIL}-2-HIDROXI-2-TRIFLUOROMETIL- PROPIONILAMINO} -FTALIDA. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA QUE COMPRENDE EL COMPUESTO UNO DONDE LA DOSIS DIARIA ES ENTRE 0,01mg Y 2 mg Y COMPRENDER ADEMAS UNA CANTIDAD DE 17O-ETINIL ESTRADIOL U OTRO COMPONENTE ESTROGENICO. UN COMPUESTO PREFERIDO ES (+)-5-{2-HIDROXI-3-[1-(2-FLUORO-5-TRIFLUOROMETILFENIL)-CICLOPROPIL]-2-TRIFLUOROMETIL- PROPIONILAMINO} -FTALIDA O UN DERIVADO O ANALOGO DEL MISMO. LAS PROGESTINA DE LA PRESENTE INVENCION EN COMBINACION CON ESTROGENOS PUEDEN SER UTILES EN LA CONTRACEPCION, TERAPIA DE REEMPLAZO HORMONAL Y TRASTORNOS GINECOLOGICOS
PE2003000244A 2002-03-11 2003-03-11 Progestinas no esteroides PE20040157A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36304402P 2002-03-11 2002-03-11
EP02005530A EP1344776A1 (en) 2002-03-11 2002-03-11 5- 2-hydroxy-3-[1-(3-trifluoromethylphenyl)-cyclopropyl]-propionylamino -phtalide and 6- 2-hydroxy-3-[1-(3-trifluoromethylphenyl)-cyclopropyl]-propionylamino -4-methyl-2,3-benzoxazin-1-one derivatives with progesterone receptor modulating activity for use in fertility control, hormone replacement therapy and the treatment of gynecological disorders

Publications (1)

Publication Number Publication Date
PE20040157A1 true PE20040157A1 (es) 2004-06-03

Family

ID=27806515

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003000244A PE20040157A1 (es) 2002-03-11 2003-03-11 Progestinas no esteroides

Country Status (26)

Country Link
US (1) US7388006B2 (es)
EP (1) EP1482925B1 (es)
JP (1) JP2005526064A (es)
CN (1) CN1652768A (es)
AR (1) AR035904A1 (es)
AU (1) AU2003209720A1 (es)
BR (1) BR0308394A (es)
CA (1) CA2478948A1 (es)
CR (1) CR7490A (es)
DE (1) DE60311236T2 (es)
DK (1) DK1482925T3 (es)
ES (1) ES2280766T3 (es)
HR (1) HRP20040923A2 (es)
IL (1) IL164032A0 (es)
MX (1) MXPA04008881A (es)
NO (1) NO20044279L (es)
NZ (1) NZ535427A (es)
PE (1) PE20040157A1 (es)
PL (1) PL372490A1 (es)
PT (1) PT1482925E (es)
RS (1) RS89504A (es)
RU (1) RU2314299C2 (es)
TW (1) TW200307674A (es)
UA (1) UA78027C2 (es)
UY (1) UY27715A1 (es)
WO (1) WO2003075915A1 (es)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102004062182B4 (de) * 2004-12-20 2007-06-06 Bayer Schering Pharma Ag Transdermales Pflaster mit Progesteron A-Spezifische Liganden (PRASL) als Wirkstoff
US20070015689A1 (en) * 2005-06-23 2007-01-18 Alza Corporation Complexation of metal ions with polypeptides
US7408060B2 (en) 2005-06-24 2008-08-05 Schering Ag Nonsteroidal progesterone receptor modulators
DE102005030294A1 (de) * 2005-06-24 2007-01-04 Schering Ag Nichtsteroidale Progesteronrezeptor-Modulatoren
US7261742B2 (en) 2005-10-13 2007-08-28 S.C. Johnson & Son, Inc. Method of deodorizing a textile
AU2006324097B2 (en) * 2005-12-09 2011-08-25 F. Hoffmann-La Roche Ag Glucocorticoid receptor modulators as antiinflammatory agents
EP1960351B1 (en) * 2005-12-09 2013-06-19 F.Hoffmann-La Roche Ag Propionamide compounds as antiinflammatory agents
DE102006061913A1 (de) * 2006-12-21 2008-06-26 Bayer Schering Pharma Aktiengesellschaft Nichtsteroidale Progesteronrezeptor-Modulatoren
UY30805A1 (es) * 2006-12-21 2008-07-31 Bayer Schering Pharma Ag Moduladores no esteroides de receptores de progesterona
CN101289408B (zh) * 2007-04-18 2013-02-27 中国科学院上海药物研究所 非甾体类孕激素受体调节剂及其制备方法、药物组合物和用途
DE102007032800A1 (de) 2007-07-10 2009-01-15 Bayer Schering Pharma Aktiengesellschaft Nichtsteroidale Progesteronrezeptor-Modulatoren
DE102007058747A1 (de) * 2007-12-05 2009-06-10 Bayer Schering Pharma Aktiengesellschaft Nichtsteroidale Progesteronrezeptor-Modulatoren
CA2710293A1 (en) * 2007-12-20 2009-07-02 Teva Women's Health, Inc. Dosage regimens and pharmaceutical compositions and packages for emergency contraception
EP3936133A1 (en) 2011-11-23 2022-01-12 TherapeuticsMD, Inc. Natural combination hormone replacement formulations and therapies
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US20150196640A1 (en) 2012-06-18 2015-07-16 Therapeuticsmd, Inc. Progesterone formulations having a desirable pk profile
US10806697B2 (en) 2012-12-21 2020-10-20 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US20130338122A1 (en) 2012-06-18 2013-12-19 Therapeuticsmd, Inc. Transdermal hormone replacement therapies
US10471072B2 (en) 2012-12-21 2019-11-12 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10537581B2 (en) 2012-12-21 2020-01-21 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11266661B2 (en) 2012-12-21 2022-03-08 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10568891B2 (en) 2012-12-21 2020-02-25 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US9180091B2 (en) 2012-12-21 2015-11-10 Therapeuticsmd, Inc. Soluble estradiol capsule for vaginal insertion
US11246875B2 (en) 2012-12-21 2022-02-15 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
CN105764491A (zh) 2013-12-09 2016-07-13 度瑞公司 药物活性剂复合物、聚合物复合物,以及包括其的组合物和方法
US10206932B2 (en) 2014-05-22 2019-02-19 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US10328087B2 (en) 2015-07-23 2019-06-25 Therapeuticsmd, Inc. Formulations for solubilizing hormones
CA3020153A1 (en) 2016-04-01 2017-10-05 Therapeuticsmd, Inc. Steroid hormone pharmaceutical composition
US10286077B2 (en) 2016-04-01 2019-05-14 Therapeuticsmd, Inc. Steroid hormone compositions in medium chain oils
EP3622266B1 (en) * 2017-05-10 2022-08-17 Ventana Medical Systems, Inc. Stabilized two-part hematoxylin solution utilizing ph adjustment, method for staining and kit
US11633405B2 (en) 2020-02-07 2023-04-25 Therapeuticsmd, Inc. Steroid hormone pharmaceutical formulations

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8617653D0 (en) * 1986-07-18 1986-08-28 Ici Plc Amide derivatives
DE19723722A1 (de) * 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
US6245804B1 (en) * 1997-05-30 2001-06-12 Schering Aktiengesellschaft Nonsteroidal gestagens
NO312255B1 (no) * 2000-06-28 2002-04-15 Pgs Reservoir Consultants As Verktöy for gjennomhulling av et langsgående veggparti av et fôringsrör
DE10038639A1 (de) * 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
WO2002054064A2 (en) * 2000-12-28 2002-07-11 Schering Ag Method for screening for progesterone receptor isoform-specific ligands

Also Published As

Publication number Publication date
CA2478948A1 (en) 2003-09-18
PL372490A1 (en) 2005-07-25
TW200307674A (en) 2003-12-16
JP2005526064A (ja) 2005-09-02
UA78027C2 (en) 2007-02-15
NZ535427A (en) 2006-08-31
RU2314299C2 (ru) 2008-01-10
AU2003209720A1 (en) 2003-09-22
US7388006B2 (en) 2008-06-17
IL164032A0 (en) 2005-12-18
ES2280766T3 (es) 2007-09-16
CR7490A (es) 2006-02-07
DK1482925T3 (da) 2007-05-14
NO20044279L (no) 2004-12-08
RU2004130430A (ru) 2005-08-10
US20030232824A1 (en) 2003-12-18
CN1652768A (zh) 2005-08-10
EP1482925A1 (en) 2004-12-08
UY27715A1 (es) 2003-08-29
BR0308394A (pt) 2005-01-25
MXPA04008881A (es) 2004-12-07
PT1482925E (pt) 2007-04-30
HRP20040923A2 (en) 2004-12-31
DE60311236D1 (de) 2007-03-08
AR035904A1 (es) 2004-07-28
RS89504A (sr) 2006-10-27
EP1482925B1 (en) 2007-01-17
WO2003075915A1 (en) 2003-09-18
DE60311236T2 (de) 2008-02-14

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