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
EP02005530.7 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 (2)

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

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Family Applications (1)

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

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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
WO2007065828A1 (en) * 2005-12-09 2007-06-14 F. Hoffmann-La Roche Ag Glucocorticoid receptor modulators as antiinflammatory agents
UY30805A1 (es) * 2006-12-21 2008-07-31 Bayer Schering Pharma Ag Moduladores no esteroides de receptores de progesterona
DE102006061913A1 (de) * 2006-12-21 2008-06-26 Bayer Schering Pharma Aktiengesellschaft Nichtsteroidale Progesteronrezeptor-Modulatoren
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
EA201070715A1 (ru) * 2007-12-20 2011-02-28 Тева Вимен'С Хелс, Инк. Режимы дозирования, фармацевтические композиции и упаковки для экстренной контрацепции
RS62297B1 (sr) 2011-11-23 2021-09-30 Therapeuticsmd Inc Prirodne kombinovane hormonske supstitucione formulacije i terapije
US9301920B2 (en) 2012-06-18 2016-04-05 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
US10806740B2 (en) 2012-06-18 2020-10-20 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
US20130338122A1 (en) 2012-06-18 2013-12-19 Therapeuticsmd, Inc. Transdermal hormone replacement therapies
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
US11246875B2 (en) 2012-12-21 2022-02-15 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
US9180091B2 (en) 2012-12-21 2015-11-10 Therapeuticsmd, Inc. Soluble estradiol capsule for vaginal insertion
US10537581B2 (en) 2012-12-21 2020-01-21 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US20160303242A1 (en) 2013-12-09 2016-10-20 Durect Corporation Pharmaceutically Active Agent Complexes, Polymer Complexes, and Compositions and Methods Involving the Same
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
US9931349B2 (en) 2016-04-01 2018-04-03 Therapeuticsmd, Inc. Steroid hormone pharmaceutical composition
US10286077B2 (en) 2016-04-01 2019-05-14 Therapeuticsmd, Inc. Steroid hormone compositions in medium chain oils
CA3062732C (en) 2017-05-10 2023-08-01 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

Citations (2)

* Cited by examiner, † Cited by third party
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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GB8617653D0 (en) * 1986-07-18 1986-08-28 Ici Plc Amide derivatives
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
JP2004516841A (ja) * 2000-12-28 2004-06-10 シエーリング アクチエンゲゼルシャフト プロゲステロンレセプターアイソフォーム特異的リガンドおよび組織選択的プロゲステロンレセプターリガンドについてスクリーニングする方法

Patent Citations (2)

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

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MM4A The patent is invalid due to non-payment of fees

Effective date: 20080311