RU2314299C2 - 5-{2-гидрокси-3-[1-(3-трифторметилфенил)циклопропил]пропиониламино}-фталид и родственные соединения, обладающие модулирующей активностью в отношении рецептора прогестерона, для применения при контроле репродуктивной функции и гормонзаместительной терапии - Google Patents

5-{2-гидрокси-3-[1-(3-трифторметилфенил)циклопропил]пропиониламино}-фталид и родственные соединения, обладающие модулирующей активностью в отношении рецептора прогестерона, для применения при контроле репродуктивной функции и гормонзаместительной терапии Download PDF

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Publication number
RU2314299C2
RU2314299C2 RU2004130430/04A RU2004130430A RU2314299C2 RU 2314299 C2 RU2314299 C2 RU 2314299C2 RU 2004130430/04 A RU2004130430/04 A RU 2004130430/04A RU 2004130430 A RU2004130430 A RU 2004130430A RU 2314299 C2 RU2314299 C2 RU 2314299C2
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RU
Russia
Prior art keywords
trifluoromethylphenyl
cyclopropyl
hydroxy
fluoro
trifluoromethylpropionylamino
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RU2004130430/04A
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English (en)
Russian (ru)
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RU2004130430A (ru
Inventor
Норберт ШМЕЕС (DE)
Норберт Шмеес
Манфред ЛЕМАНН (DE)
Манфред Леманн
Ульрике ФУРМАНН (DE)
Ульрике Фурманн
Петер МУН (DE)
Петер Мун
Криста ХЕГЕЛЕ-ХАРТУНГ (DE)
Криста Хегеле-Хартунг
Михаэль КЛОТЦБЮХЕР (DE)
Михаэль КЛОТЦБЮХЕР
Original Assignee
Шеринг Акциенгезельшафт
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Priority claimed from EP02005530A external-priority patent/EP1344776A1/en
Application filed by Шеринг Акциенгезельшафт filed Critical Шеринг Акциенгезельшафт
Publication of RU2004130430A publication Critical patent/RU2004130430A/ru
Application granted granted Critical
Publication of RU2314299C2 publication Critical patent/RU2314299C2/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic 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
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88—Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • 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
    • A61K31/565—Compounds 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/02—1,2-Oxazines; Hydrogenated 1,2-oxazines

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  • 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)
RU2004130430/04A 2002-03-11 2003-03-10 5-{2-гидрокси-3-[1-(3-трифторметилфенил)циклопропил]пропиониламино}-фталид и родственные соединения, обладающие модулирующей активностью в отношении рецептора прогестерона, для применения при контроле репродуктивной функции и гормонзаместительной терапии RU2314299C2 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US36304402P 2002-03-11 2002-03-11
US60/363,044 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
EP02005530.7 2002-03-11

Publications (2)

Publication Number Publication Date
RU2004130430A RU2004130430A (ru) 2005-08-10
RU2314299C2 true RU2314299C2 (ru) 2008-01-10

Family

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Application Number Title Priority Date Filing Date
RU2004130430/04A RU2314299C2 (ru) 2002-03-11 2003-03-10 5-{2-гидрокси-3-[1-(3-трифторметилфенил)циклопропил]пропиониламино}-фталид и родственные соединения, обладающие модулирующей активностью в отношении рецептора прогестерона, для применения при контроле репродуктивной функции и гормонзаместительной терапии

Country Status (26)

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

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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
AU2006324090B2 (en) * 2005-12-09 2012-05-31 F. Hoffmann-La Roche Ag Propionamide compounds as antiinflammatory agents
BRPI0619518A2 (pt) * 2005-12-09 2011-10-11 Hoffmann La Roche moduladores do receptor de glicocorticoide, composição farmacêutica que os compreende e usos dos mesmos
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
BRPI0819571A2 (pt) * 2007-12-20 2019-09-24 Teva Womenss Health Inc "método para contracepção de emergência, pacote farmacêutico para contracepção de emergência e composição farmacêutica"
BR112014012444B1 (pt) 2011-11-23 2021-12-14 Therapeuticsmd, Inc Composição farmacêutica compreendendo estradiol solubilizado, progesterona e um agente de solubilização, bem como usos desta para tratar um sintoma relacionado à menopausa em uma mulher
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US20130338122A1 (en) 2012-06-18 2013-12-19 Therapeuticsmd, Inc. Transdermal hormone replacement therapies
US20150196640A1 (en) 2012-06-18 2015-07-16 Therapeuticsmd, Inc. Progesterone formulations having a desirable pk profile
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US10806697B2 (en) 2012-12-21 2020-10-20 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
US11266661B2 (en) 2012-12-21 2022-03-08 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
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
US11246875B2 (en) 2012-12-21 2022-02-15 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
JP6564369B2 (ja) 2013-12-09 2019-08-21 デュレクト コーポレイション 薬学的活性剤複合体、ポリマー複合体、ならびにこれらを伴う組成物及び方法
RU2016143081A (ru) 2014-05-22 2018-06-26 Терапьютиксмд, Инк. Натуральные комбинированные гормонозаместительные составы и терапии
US10328087B2 (en) 2015-07-23 2019-06-25 Therapeuticsmd, Inc. Formulations for solubilizing hormones
US10286077B2 (en) 2016-04-01 2019-05-14 Therapeuticsmd, Inc. Steroid hormone compositions in medium chain oils
US9931349B2 (en) 2016-04-01 2018-04-03 Therapeuticsmd, Inc. Steroid hormone pharmaceutical composition
WO2018206521A1 (en) * 2017-05-10 2018-11-15 Ventana Medical Systems, Inc. STABILIZED TWO-PART HEMATOXYLIN SOLUTION UTILIZING pH ADJUSTMENT
US11633405B2 (en) 2020-02-07 2023-04-25 Therapeuticsmd, Inc. Steroid hormone pharmaceutical formulations

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Publication number Priority date Publication date Assignee Title
WO1998054159A1 (de) * 1997-05-30 1998-12-03 Schering Aktiengesellschaft Nichtsteroidale (hetero)zyklisch-substituierte acylanilide mit gemischter gestagener und androgener wirksamkeit
WO2002010143A1 (de) * 2000-07-28 2002-02-07 Schering Aktiengesellschaft Nichtsteroidale entzündungshemmer

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NO312255B1 (no) * 2000-06-28 2002-04-15 Pgs Reservoir Consultants As Verktöy for gjennomhulling av et langsgående veggparti av et fôringsrör
WO2002054064A2 (en) * 2000-12-28 2002-07-11 Schering Ag Method for screening for progesterone receptor isoform-specific ligands

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
WO1998054159A1 (de) * 1997-05-30 1998-12-03 Schering Aktiengesellschaft Nichtsteroidale (hetero)zyklisch-substituierte acylanilide mit gemischter gestagener und androgener wirksamkeit
WO2002010143A1 (de) * 2000-07-28 2002-02-07 Schering Aktiengesellschaft Nichtsteroidale entzündungshemmer

Also Published As

Publication number Publication date
UA78027C2 (en) 2007-02-15
US7388006B2 (en) 2008-06-17
MXPA04008881A (es) 2004-12-07
BR0308394A (pt) 2005-01-25
WO2003075915A1 (en) 2003-09-18
TW200307674A (en) 2003-12-16
AR035904A1 (es) 2004-07-28
NZ535427A (en) 2006-08-31
IL164032A0 (en) 2005-12-18
AU2003209720A1 (en) 2003-09-22
HRP20040923A2 (en) 2004-12-31
PL372490A1 (en) 2005-07-25
DK1482925T3 (da) 2007-05-14
PE20040157A1 (es) 2004-06-03
RU2004130430A (ru) 2005-08-10
US20030232824A1 (en) 2003-12-18
CA2478948A1 (en) 2003-09-18
DE60311236D1 (de) 2007-03-08
JP2005526064A (ja) 2005-09-02
CR7490A (es) 2006-02-07
DE60311236T2 (de) 2008-02-14
PT1482925E (pt) 2007-04-30
CN1652768A (zh) 2005-08-10
EP1482925A1 (en) 2004-12-08
NO20044279L (no) 2004-12-08
EP1482925B1 (en) 2007-01-17
ES2280766T3 (es) 2007-09-16
RS89504A (sr) 2006-10-27
UY27715A1 (es) 2003-08-29

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Effective date: 20080311