DE60311236T2 - 5-(2-hydroxy-3-'1-(3-trifluormethylphenyl)-cycloproplü-propionylamino)-phtalid und verwandte verbindungen mit progesteron-rezeptor-modulierender wirkung zur verwendung bei der fertilitätskontrolle und hormonersatztherapie - Google Patents
5-(2-hydroxy-3-'1-(3-trifluormethylphenyl)-cycloproplü-propionylamino)-phtalid und verwandte verbindungen mit progesteron-rezeptor-modulierender wirkung zur verwendung bei der fertilitätskontrolle und hormonersatztherapie Download PDFInfo
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- DE60311236T2 DE60311236T2 DE60311236T DE60311236T DE60311236T2 DE 60311236 T2 DE60311236 T2 DE 60311236T2 DE 60311236 T DE60311236 T DE 60311236T DE 60311236 T DE60311236 T DE 60311236T DE 60311236 T2 DE60311236 T2 DE 60311236T2
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- Prior art keywords
- cyclopropyl
- hydroxy
- trifluoromethylphenyl
- fluoro
- compound
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- 229920002379 silicone rubber Polymers 0.000 description 1
- 239000004945 silicone rubber Substances 0.000 description 1
- 229940054269 sodium pyruvate Drugs 0.000 description 1
- 239000008137 solubility enhancer Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 229960005322 streptomycin Drugs 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
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- 230000002459 sustained effect Effects 0.000 description 1
- 230000035900 sweating Effects 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
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- 235000012222 talc Nutrition 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 210000001541 thymus gland Anatomy 0.000 description 1
- 125000005490 tosylate group Chemical group 0.000 description 1
- 230000014616 translation Effects 0.000 description 1
- MWKJTNBSKNUMFN-UHFFFAOYSA-N trifluoromethyltrimethylsilane Chemical compound C[Si](C)(C)C(F)(F)F MWKJTNBSKNUMFN-UHFFFAOYSA-N 0.000 description 1
- 230000001836 utereotrophic effect Effects 0.000 description 1
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Classifications
-
- 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
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)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36304402P | 2002-03-11 | 2002-03-11 | |
| US363044P | 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 | 2002-03-11 | ||
| 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 |
|---|---|
| DE60311236D1 DE60311236D1 (de) | 2007-03-08 |
| DE60311236T2 true DE60311236T2 (de) | 2008-02-14 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60311236T Expired - Fee Related DE60311236T2 (de) | 2002-03-11 | 2003-03-10 | 5-(2-hydroxy-3-'1-(3-trifluormethylphenyl)-cycloproplü-propionylamino)-phtalid und verwandte verbindungen mit progesteron-rezeptor-modulierender wirkung zur verwendung bei der fertilitätskontrolle und hormonersatztherapie |
Country Status (26)
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| 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=) |
Families Citing this family (32)
| 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 |
| 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 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8617653D0 (en) * | 1986-07-18 | 1986-08-28 | Ici Plc | Amide derivatives |
| US6245804B1 (en) * | 1997-05-30 | 2001-06-12 | Schering Aktiengesellschaft | Nonsteroidal gestagens |
| DE19723722A1 (de) * | 1997-05-30 | 1998-12-10 | Schering Ag | Nichtsteroidale Gestagene |
| 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 |
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2003
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- 2003-03-10 IL IL16403203A patent/IL164032A0/xx unknown
- 2003-03-10 CA CA002478948A patent/CA2478948A1/en not_active Abandoned
- 2003-03-10 PT PT03743862T patent/PT1482925E/pt unknown
- 2003-03-10 HR HRP20040923 patent/HRP20040923A2/hr not_active Application Discontinuation
- 2003-03-10 DK DK03743862T patent/DK1482925T3/da active
- 2003-03-10 WO PCT/EP2003/002441 patent/WO2003075915A1/en not_active Ceased
- 2003-03-10 ES ES03743862T patent/ES2280766T3/es not_active Expired - Lifetime
- 2003-03-10 DE DE60311236T patent/DE60311236T2/de not_active Expired - Fee Related
- 2003-03-10 BR BR0308394-2A patent/BR0308394A/pt not_active IP Right Cessation
- 2003-03-10 MX MXPA04008881A patent/MXPA04008881A/es not_active Application Discontinuation
- 2003-03-10 AU AU2003209720A patent/AU2003209720A1/en not_active Abandoned
- 2003-03-10 NZ NZ535427A patent/NZ535427A/en unknown
- 2003-03-10 CN CNA038106590A patent/CN1652768A/zh active Pending
- 2003-03-10 RU RU2004130430/04A patent/RU2314299C2/ru not_active IP Right Cessation
- 2003-03-10 EP EP03743862A patent/EP1482925B1/en not_active Expired - Lifetime
- 2003-03-10 RS YU89504A patent/RS89504A/sr unknown
- 2003-03-10 PL PL03372490A patent/PL372490A1/xx not_active Application Discontinuation
- 2003-03-11 PE PE2003000244A patent/PE20040157A1/es not_active Application Discontinuation
- 2003-03-11 TW TW092105213A patent/TW200307674A/zh unknown
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- 2003-10-03 UA UA20041008153A patent/UA78027C2/uk unknown
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2004
- 2004-09-21 CR CR7490A patent/CR7490A/es not_active Application Discontinuation
- 2004-10-08 NO NO20044279A patent/NO20044279L/no not_active Application Discontinuation
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 |
| JP2005526064A (ja) | 2005-09-02 |
| CR7490A (es) | 2006-02-07 |
| 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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|---|---|---|---|
| 8327 | Change in the person/name/address of the patent owner |
Owner name: BAYER SCHERING PHARMA AG, 13353 BERLIN, DE |
|
| 8364 | No opposition during term of opposition | ||
| 8327 | Change in the person/name/address of the patent owner |
Owner name: BAYER SCHERING PHARMA AKIENGESELLSCHAFT, 13353, DE |
|
| 8339 | Ceased/non-payment of the annual fee |