JP2005526064A - 受精能制御およびホルモン置換療法における使用のためのプロゲステロン受容体調整活性を有する５−｛２−ヒドロキシ−３−１−（３−トリフルオロメチルフェニル）−シクロプロピル−プロピオニルアミノ｝−フタリドおよび関連化合物 - Google Patents

受精能制御およびホルモン置換療法における使用のためのプロゲステロン受容体調整活性を有する５−｛２−ヒドロキシ−３−１−（３−トリフルオロメチルフェニル）−シクロプロピル−プロピオニルアミノ｝−フタリドおよび関連化合物 Download PDF

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JP2005526064A
JP2005526064A JP2003574190A JP2003574190A JP2005526064A JP 2005526064 A JP2005526064 A JP 2005526064A JP 2003574190 A JP2003574190 A JP 2003574190A JP 2003574190 A JP2003574190 A JP 2003574190A JP 2005526064 A JP2005526064 A JP 2005526064A
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compound
cyclopropyl
trifluoromethylphenyl
propionylamino
hydroxy
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Japanese (ja)
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JP2005526064A5 (https=
Inventor
シュメース，ノルベルト
レーマン，マンフレット
フュールマン，ウルリケ
ムーン，ペーター
ヘゲレ−ハルトゥンク，クリスタ
クロッツビュッハー，ミハエル
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シエーリング アクチエンゲゼルシャフト
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Priority claimed from EP02005530A external-priority patent/EP1344776A1/en
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Publication of JP2005526064A publication Critical patent/JP2005526064A/ja
Publication of JP2005526064A5 publication Critical patent/JP2005526064A5/ja
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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)
JP2003574190A 2002-03-11 2003-03-10 受精能制御およびホルモン置換療法における使用のためのプロゲステロン受容体調整活性を有する５−｛２−ヒドロキシ−３−１−（３−トリフルオロメチルフェニル）−シクロプロピル−プロピオニルアミノ｝−フタリドおよび関連化合物 Pending JP2005526064A (ja)

Applications Claiming Priority (3)

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
PCT/EP2003/002441 WO2003075915A1 (en) 2002-03-11 2003-03-10 5-}2-hydroxy-3-`1-(3-trifluoromethylphenyl)-cyclopropyl!-propionylamino}- phtalide and related compounds with progesterone receptor modulating activity for use in fertility control and hormone replacement therapy

Publications (2)

Publication Number Publication Date
JP2005526064A true JP2005526064A (ja) 2005-09-02
JP2005526064A5 JP2005526064A5 (https=) 2006-04-27

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JP2003574190A Pending JP2005526064A (ja) 2002-03-11 2003-03-10 受精能制御およびホルモン置換療法における使用のためのプロゲステロン受容体調整活性を有する５−｛２−ヒドロキシ−３−１−（３−トリフルオロメチルフェニル）−シクロプロピル−プロピオニルアミノ｝−フタリドおよび関連化合物

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=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009518353A (ja) * 2005-12-09 2009-05-07 エフ．ホフマン−ラ ロシュ アーゲー 抗炎症剤としてのグルココルチコイド受容体モジュレーター
JP2009518352A (ja) * 2005-12-09 2009-05-07 エフ．ホフマン−ラ ロシュ アーゲー 抗炎症性剤としてのプロピオンアミド化合物
JP2020519876A (ja) * 2017-05-10 2020-07-02 ヴェンタナ メディカル システムズ， インク． ｐＨ調整を利用する安定化した２パートヘマトキシリン溶液

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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
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
US11633405B2 (en) 2020-02-07 2023-04-25 Therapeuticsmd, Inc. Steroid hormone pharmaceutical formulations

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JPS6330457A (ja) * 1986-07-18 1988-02-09 インペリアル・ケミカル・インダストリ−ズ・ピ−エルシ− アシルアニリド、その製造法及びこれを含有し抗アンドロゲン作用又は月経前期作用を有する製薬組成物
WO2002001043A1 (en) * 2000-06-28 2002-01-03 Pgs Reservoir Consultants As Method and device for performing a portion of casing in a reservoir
JP2002502385A (ja) * 1997-05-30 2002-01-22 シエーリング アクチエンゲゼルシヤフト ゲスターゲン及びアンドロゲン混合作用を有する非ステロイド系（複素）環式置換アシルアニリド
WO2002054064A2 (en) * 2000-12-28 2002-07-11 Schering Ag Method for screening for progesterone receptor isoform-specific ligands

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US6245804B1 (en) * 1997-05-30 2001-06-12 Schering Aktiengesellschaft Nonsteroidal gestagens
DE10038639A1 (de) * 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer

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JPS6330457A (ja) * 1986-07-18 1988-02-09 インペリアル・ケミカル・インダストリ−ズ・ピ−エルシ− アシルアニリド、その製造法及びこれを含有し抗アンドロゲン作用又は月経前期作用を有する製薬組成物
JP2002502385A (ja) * 1997-05-30 2002-01-22 シエーリング アクチエンゲゼルシヤフト ゲスターゲン及びアンドロゲン混合作用を有する非ステロイド系（複素）環式置換アシルアニリド
WO2002001043A1 (en) * 2000-06-28 2002-01-03 Pgs Reservoir Consultants As Method and device for performing a portion of casing in a reservoir
WO2002054064A2 (en) * 2000-12-28 2002-07-11 Schering Ag Method for screening for progesterone receptor isoform-specific ligands

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009518353A (ja) * 2005-12-09 2009-05-07 エフ．ホフマン−ラ ロシュ アーゲー 抗炎症剤としてのグルココルチコイド受容体モジュレーター
JP2009518352A (ja) * 2005-12-09 2009-05-07 エフ．ホフマン−ラ ロシュ アーゲー 抗炎症性剤としてのプロピオンアミド化合物
JP2020519876A (ja) * 2017-05-10 2020-07-02 ヴェンタナ メディカル システムズ， インク． ｐＨ調整を利用する安定化した２パートヘマトキシリン溶液
US12474240B2 (en) 2017-05-10 2025-11-18 Ventana Medical Systems, Inc. Stabilized two-part hematoxylin solution utilizing pH adjustment

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
RU2314299C2 (ru) 2008-01-10
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
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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